NEW TYROSINE DERIVATIVES AS PPARy MODULATORS

ABSTRACT

Compounds of general formula I, 
     
       
         
         
             
             
         
       
     
     and the salts and solvates thereof, wherein R1 represents the radical 2-benzoylphenylamino; R2 represents —(CH 2 ) s —N(COR3)-A-J-T or —(CH 2 ) s —N(R4)-B-J-T; and s, R3, R4, A, B, J and T have the meanings disclosed herein. These compounds are PPARγ modulators and, therefore, are useful for the treatment or prevention of a condition or a disease mediated by these receptors.

CROSS-REFERENCE TO RELATED APPLICATIONS

The present application is a continuation of U.S. patent application Ser. No. 11/658,856 filed on 29 Jan. 2007 which in turn is a national stage filing under 35 U.S.C. §371 of PCT/EP2005/053728, filed on 29 Jul. 2005 which in turn claims priority under 35 U.S.C. §119 to Spanish patent application Serial No. 200401966 filed on 30 Jul. 2004.

The present invention relates to new tyrosine derivatives acting as PPARγ modulators, as well as to processes and intermediates useful for their preparation, to pharmaceutical compositions containing them and their application in medicine.

BACKGROUND ART

Peroxisome proliferator activated receptors (PPARs) belong to the superfamily of transcription factors known as nuclear receptors. This family includes steroid, retinoid and thyroid hormone receptors. Three sub-types of PPARs have been identified in humans, rodents and Xenopus laevis. They are PPARα, PPARβ/δ and PPARγ, each encoded by a different gene and showing different tissue distribution.

The gene encoding for PPARγ is transcribed in humans in three different mRNA isoforms (PPARγ1, PPARγ2 and PPARγ3) through different splicing and promoter usage (Fajas et al., J. Biol. Chem. 1997, vol. 272, p. 18779-18789). The PPARγ1 isoform shows a wide tissular distribution, while PPARγ2 and PPARγ3 are confined to certain tissues: PPARγ2 is expressed only in adipose tissue and PPARγ3 in adipose tissue as well as in macrophages (Fajas et al., FEBS Lett. 1998, vol. 438, p. 55-60).

Differences detected in tissue distribution as well as in the activation profile of the PPARγ isoforms suggest they are involved in a variety of physiological functions playing a central role in glucose homeostasis and lipid metabolism (Vamecq et al., Lancet 1999, vol. 354, p. 141-148). These functions include, for example, lipidic transport in plasma and catabolism of fatty acids, regulation of insulin sensitivity and blood glucose levels, differentiation of macrophages that form atherosclerotic plaques, inflammatory response, carcinogenesis, hyperplasia, and adipocyte differentiation, the latter being the most verified function of the PPARγ (Grimaldi, Prog. Lipid Res. 2001, vol. 40, p. 269-281; Schiller et al., J. Biol. Chem. 2001, vol. 276, p. 14133-14137). Thus, the discovery of these transcription factors has provided new pharmacological targets for the development of useful therapeutic agents for the prevention and treatment of metabolic diseases such as diabetes, obesity and dyslipidaemia.

Non-insulin dependent diabetes mellitus (NIDDM) or type 2 diabetes is characterized by an insulin resistance in peripheral tissues, including muscle, liver, and adipose tissue. Glitazones, selective PPARγ agonist compounds, are drugs that reduce insulin resistance and lower blood glucose levels. Currently two products belonging to this family, rosiglitazone and pioglitazone, have been approved for the treatment of type 2 diabetes in humans.

A great effort has been made in recent years to design new drugs that improve the side effect profile of the first glitazones, show a greater affinity as a PPARγ ligands, and increase their potency in type 2 diabetes. This rational design has yielded structurally diverse compounds that show great potency and selectivity (e.g. farglitazar).

PPARγ agonists have had shortcomings which have so far detracted from their attractiveness, such as liver toxicity (especially troglitazone), weigh gain, edema, heart weight gain (in rodents) and adiposity, as well as modest efficacy in monotherapy for type 2 diabetes. These facts have provided an incentive to develop improved insulin sensitizers.

Compounds totally or partially blocking PPARγ activity have demonstrated to inhibit adipocyte differentiation. Thus, full antagonists constitute an effective treatment for obesity. Moreover, compounds that are partial agonists in addition of being antagonists may be particularly desirable because they are effective in treating not only obesity but also in controlling hyperglycemia. The PPARγ antagonists/partial agonists are therefore effective in treating obesity and other symptoms that generally occur in non-insulin dependent diabetes, such as elevated plasma levels of glucose, tryglicerides, and insulin.

Recently, there have been reports of compounds that are PPARγ antagonists or partial agonists (WO01/30343, WO02/08188, WO2004/020408), which are useful for the treatment of obesity and type 2 diabetes, with reduced side effects (Berger et al., Trends Pharmacol. Sci. 2005, vol. 26, p. 244-51).

Examples of partial agonists in clinical development for diabetes are (−)-halofenate (metaglidasen), FK 614 (Minoura et al., Eur. J. Pharmacol. 2004, vol. 494, p. 273-8), T131 (Li et al., 64th Annu. Meet. Sci. Sess. Am. Diabetes Assoc. (June 4-June 8, Orlando) 2004, Abst 659-P), LY818 (Reifel-Miller et al., Diabetes 2003, 52 (Suppl. 1): Abst 614-P) and telmisartan, an angiotensin II blocker approved for the treatment of hypertension, with PPAR partial agonistic activity at concentrations achievable at plasmatic levels during treatment (Kurtz et al., Acta Diabetol. 2005; vol. 42 Suppl 1: S 9-16) which are currently in phase II of clinical development.

In Henkel et al., J. Med. Chem. 1998, vol. 41, p. 5020-5036; Collins et al., J. Med. Chem. 1998, vol. 41, p. 5037-5054; Cobb et al., J. Med. Chem. 1998, vol. 41, p. 5055-5069, WO 94/29285 and in WO 97/31907 de N-(2-benzoylphenyl)-L-tyrosine derivatives are described as being potent and selective PPARγ agonists. Documents WO 03/011814 and WO 03/011834 disclose N-(2-benzoylphenyl)-L-tyrosine derivatives as partial PPARγ agonists. Document U.S. Pat. No. 6,274,608 describes N-(2-benzoylphenyl)-L-tyrosine derivatives as being useful in the treatment and/or prevention of conditions mediated by Retinoid X Receptor (RXR) and the PPAR families.

Obviously, it is of great interest to provide new therapeutic agents that modulate PPARγ.

SUMMARY OF THE INVENTION

One aspect of the present invention relates to the provision of new compounds of general formula I,

their stereoisomers and mixtures thereof, their polymorphs and mixtures thereof, and the pharmaceutically acceptable solvates and addition salts of all of them, wherein R1 represents the radical 2-benzoylphenylamino; R2 represents —(CH₂)_(s)—N(COR3)-A-J-T or —(CH₂)_(s)—N(R4)-B-J-T; R3 represents —(C₁-C₁₀)alkyl optionally substituted by one or more substituents selected from —F, —Cl, —Br and —O(C₁-C₄)alkyl; —(C₂-C₆)alkenyl; —(C₂-C₆)alkynyl; —(C₁-C₃)alkylene-Y; —(C₂-C₃)alkenylene-Y; —(C₂-C₃)alkynylene-Y or —Y; R4 represents —(C₄-C₁₀)alkyl optionally substituted by one or more substituents selected from —F, —Cl, —Br and —O(C₁-C₄)alkyl; —(C₂-C₆)alkenyl; —(C₂-C₆)alkynyl; —(C₁-C₄)alkylene-Y; —(C₂-C₄)alkenylene-Y; —(C₂-C₄)alkynylene-Y or —Y; s represents 2 or 3; A represents —(C₁-C₄)alkylene-; —(C₂-C₄)alkenylene-; —(C₂-C₄)alkynylene-; —(C₁-C₄)alkylene-Z-, wherein the alkylene part is attached to the N atom and Z is attached to J; or -Z-; B represents —(C₄)alkylene-; —(C₂-C₄)alkenylene-; —(C₂-C₄)alkynylene-; —(C₁-C₄)alkylene-Z-, wherein the alkylene part is attached to the N atom and Z is attached to J; or -Z-; J represents a single bond or a biradical selected from the following groups:

a) —(CH₂)₁₋₄—, —O—, —S—, —SO—, —SO₂—, —CO—, —OCO—, —COO—, —OCONR5-, —NR5COO—, —CONR5-, —NR5CO—, —NR5-, —NR5SO₂—, —SO₂NR5-; and

b) —O(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-O—, —S(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-S—, —SO(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-SO—, —SO₂(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-SO₂—, —OCO—(C₁-C₄)alkyl-, —COO—(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-OCO—, —(C₁-C₄)alkyl-COO—, —OCONR5-(C₁-C₄)alkyl-, —NR5COO—(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-OCONR5-, —(C₁-C₄)alkyl-NR5COO—, —CONR5-(C₁-C₄)alkyl-, —NR5CO—(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-CONR5-, —(C₁-C₄)alkyl-NR5CO—, —NR5-(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-NR5-, —SO₂NR5-(C₁-C₄)alkyl-, —NR5SO₂—(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-SO₂NR5-, —(C₁-C₄)alkyl-NR5SO₂—;

T represents —H, —(C₁-C₄)alkyl, —(C₂-C₄)alkenyl, —(C₂-C₄)alkynyl or —Y; Y represents a monoradical coming from a cycle selected from a (C₃-C₆)cycloalkane, cyclohexene, a heterocycle, benzene and a bicycle, wherein all these cycles can be optionally substituted with one or more substituents selected from the group —OH, —CHO, —SH, —NO₂, —CN, —F, —Cl, —Br, —CO(C₁-C₄)alkyl, —COO(C₁-C₄)alkyl, —OCO(C₁-C₄)alkyl, —S(C₁-C₄)alkyl, —SO(C₁-C₄)alkyl, —SO₂(C₁-C₄)alkyl, —SO₂—O(C₁-C₄)alkyl, —O—SO₂(C₁-C₄)alkyl, —NR5R6, —CONR5R6, —(C₁-C₄)alkyl optionally substituted by one or more —OH or —F and —O(C₁-C₄)alkyl optionally substituted by one or more —OH or —F, and wherein the cycles (C₃-C₆)cycloalkane, cyclohexene and bicycle can also be optionally substituted with one or more substituents oxo (═O); Z represents a biradical coming from a cycle selected from a (C₃-C₆)cycloalkane, cyclohexene, a heterocycle, benzene and a bicycle, wherein all these cycles can be optionally substituted with one or more substituents selected from the group —OH, —CHO, —SH, —NO₂, —CN, —F, —Cl, —Br, —CO(C₁-C₄)alkyl, —COO(C₁-C₄)alkyl, —OCO(C₁-C₄)alkyl, —S(C₁-C₄)alkyl, —SO(C₁-C₄)alkyl, —SO₂(C₁-C₄)alkyl, —SO₂—O(C₁-C₄)alkyl, —O—SO₂(C₁-C₄)alkyl, —NR5R6, —CONR5R6, —(C₁-C₄)alkyl optionally substituted by one or more —OH or —F and —O(C₁-C₄)alkyl optionally substituted by one or more —OH or —F, and wherein the cycles (C₃-C₆)cycloalkane, cyclohexene and bicycle can also be optionally substituted with one or more substituents oxo (═O); R5 and R6 independently represent —H or —(C₁-C₄)alkyl;

a heterocycle in the above definitions represents a five- or six-membered aromatic ring containing from one to three heteroatoms independently selected from O, S and N, wherein said ring can be attached to the rest of the molecule through a carbon or a nitrogen atom; and

a bicycle in the above definitions represents a partially unsaturated, saturated or aromatic seven- to ten-membered ring optionally containing from one to three heteroatoms independently selected from O, S and N, wherein said ring or rings can be attached to the rest of the molecule through a carbon or a nitrogen atom.

The compounds of formula I are PPARγ modulators and, therefore, useful as active pharmaceutical substances.

Thus, another aspect of this invention relates to the pharmaceutical compositions which comprise an effective amount of a compound of formula I or a pharmaceutically acceptable salt or solvate thereof and one or more pharmaceutical acceptable excipients.

Another aspect of the present invention relates to the use of a compound of formula I for the manufacture of a medicament for the treatment or prevention of diseases mediated by PPARγ. Another aspect of the present invention relates to the use of a compound of formula I for the manufacture of a medicament for the treatment or prevention of metabolic diseases in a subject in need thereof, including a human. Another aspect of the present invention relates to the use of a compound of formula I or a pharmaceutically acceptable salt or solvate thereof for the manufacture of a medicament for the treatment or prevention of metabolic diseases selected from non-insulin-dependent diabetes mellitus and obesity in a subject in need thereof, including a human. Another aspect of the present invention relates to the use of a compound of formula I or a pharmaceutically acceptable salt or solvate thereof for the manufacture of a medicament for the treatment or prevention of cardiovascular diseases associated with metabolic syndrome, inflammatory diseases, cancer, bone diseases, skin wound healing, cutaneous disorders associated with an anomalous differentiation of epidermic cells, and other disorders where insulin resistance is a component in a subject in need thereof, including a human.

Another aspect of the present invention relates to the method for the treatment or prevention of diseases mediated by PPARγ comprising the administration to a mammal, including a human, an effective amount of a compound of formula I or a pharmaceutically acceptable salt or solvate thereof. Another aspect of the present invention relates to the method for the treatment or prevention of metabolic diseases comprising the administration to a mammal, including a human, an effective amount of a compound of formula I or a pharmaceutically acceptable salt or solvate thereof. Another aspect of the present invention relates to the method for the treatment or prevention of metabolic diseases selected from non-insulin-dependent diabetes mellitus and obesity comprising the administration to a mammal, including a human, an effective amount of a compound of formula I or a pharmaceutically acceptable salt or solvate thereof. Another aspect of the present invention relates to the method for the treatment or prevention of cardiovascular diseases associated with metabolic syndrome, inflammatory diseases, cancer, bone diseases, skin wound healing, cutaneous disorders associated with an anomalous differentiation of epidermic cells and other disorders where insulin resistance is a component, comprising the administration to a mammal, including a human, an effective amount of a compound of formula I or a pharmaceutically acceptable salt or solvate thereof.

In the previous definitions, the terms “alkyl” and “alkylene” mean respectively a monoradical or biradical straight or branched saturated hydrocarbon chain having the indicated number of carbon atoms. Examples of alkyl include, but are not limited to, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, pentyl, isopentyl, neopentyl, hexyl, heptyl, octyl, nonyl, decyl and the like.

The terms “alkenyl” and “alkenylene”, as used herein, mean respectively a monoradical or biradical straight or branched unsaturated hydrocarbon chain, having the indicated number of carbon atoms and also containing one or more double bonds. Examples of alkenyl include, but are not limited to, ethenyl, 1-propenyl, 2-propenyl, 1-butenyl, 2-butenyl, 3-butenyl, 1,3-butadienyl, 1-pentenyl, 2-pentenyl, 3-pentenyl, 4-pentenyl, 1-hexenyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, 5-hexenyl and the like.

The terms “alkynyl” and “alkynylene”, as used herein, mean respectively a monoradical or biradical straight or branched unsaturated hydrocarbon chain, having the indicated number of carbon atoms and also containing one or more triple bonds. Examples of alkynyl include, but are not limited to, ethynyl, 1-propynyl, 2-propynyl, 1-butynyl, 2-butynyl, 3-butynyl, 1,3-butadiynyl, 1-pentynyl, 2-pentynyl, 3-pentynyl, 4-pentynyl, 1-hexynyl, 2-hexynyl, 3-hexynyl, 4-hexynyl, 5-hexynyl and the like.

The term heterocycle as used herein refers to a five- or six-membered monocyclic aromatic ring containing from one to three heteroatoms independently selected from O, S and N. As mentioned previously, these heterocycles can be optionally substituted with one or more substituents, which can be placed on any available position of the cycle, and can be attached to the rest of the molecule via any available carbon or nitrogen atoms. Examples include, but are not limited to, 1,2,4-oxadiazole, 1,2,4-thiadiazole, 1,3,4-oxadiazole, 1,3,4-thiadiazole, furan, imidazole, isoxazole, isothiazole, oxazole, pyrazol, pyrrole, thiazole, thiophene, 1,2,3-triazole, 1,2,4-triazole, pyrazine, pyridazine, pyridine, pyrimidine and the like.

The term (C₃-C₆)cycloalkane as used herein refers to saturated monocyclic carbocyclic ring having the indicated number of carbon atoms. As mentioned previously, it can be optionally substituted with one or more substituents, which can be placed on any available position of the cycle. Examples of (C₃-C₆)cycloalkanes include, but are not limited to, cyclopropane, cyclobutane, cyclopentane and cyclohexane.

The term bicycle, as used herein refers to a partially unsaturated, saturated or aromatic seven- to ten-membered ring optionally containing from one to three heteroatoms independently selected from O, S and N, wherein said ring or rings can be attached to the rest of the molecule through a carbon or a nitrogen atom. As mentioned previously, it can be optionally substituted with one or more substituents, which can be placed on any available position of the cycle. Examples of bicyclic groups include, among others, naphthalene, 1,2,3,4-tetrahydronaphthalene, quinoline, 1,2,3,4-tetrahydroquinoline, isoquinoline, benzofuran, 2,3-dihydrobenzofuran, benzothiophene, indole, benzimidazole, benzotriazol, bicyclo[2.2.1]heptane, bicyclo[3.2.1]octane and bicyclo[3.2.2]nonane.

The expression “optionally substituted with one or more” means that a group can be unsubstituted or substituted with one or more, preferably with 1, 2, 3 or 4 substituents, provided that this group has 1, 2, 3 or 4 positions susceptible of being substituted.

Throughout the description and claims the word “comprise” and variations of the word, such as “comprising”, are not intended to exclude other additives, components, elements or steps. The disclosures in the abstract accompanying this application and in the application from which priority is claimed, are incorporated herein as reference.

As used therein the term “treatment” includes treatment, prevention and management of such condition. The term “pharmaceutically acceptable” as used herein refers to those compounds, compositions, and/or dosage forms which are, within the scope of medical judgement, suitable for use in contact with the tissues of humans and animals without excessive toxicity, irritation, allergic response, or other problem or complication, commensurate with a reasonable benefit/risk ratio.

Compounds of formula I of the present invention comprise at least one chiral center. The present invention includes both the racemic compounds and the enantiomeric compounds, i.e. compounds of formula Ia (wherein the configuration of the chiral carbon attached to R1 is (S)) and compounds of formula Ib (wherein the configuration of the chiral carbon attached to R1 is (R)) as shown below.

In a particular embodiment of the invention the configuration of the chiral carbon attached to R1 is (S).

In another embodiment in a compound of formula I or Ia, R2 represents —(CH₂)_(s)—N(COR3)-A-J-T. In another embodiment in a compound of formula I or Ia, R2 represents —(CH₂)_(s)—N(R4)-B-J-T. In another embodiment in a compound of formula I or Ia, J represents a single bond and T represents —H. In another embodiment in a compound of formula I or Ia, J represents —(CH₂)₁₋₄—, —O—, —S—, —SO—, —SO₂—, —O(C₁-C₄)alkyl- or —S(C₁-C₄)alkyl-. In another embodiment in a compound of formula I or Ia, T represents —H or —(C₁-C₄)alkyl.

In another embodiment in a compound of formula I or Ia, R2 represents —(CH₂)_(s)—N(COR3)-A-J-T; R3 represents —(C₁-C₁₀)alkyl optionally substituted by one or more substituents selected from —F, —Cl, —Br and —O(C₁-C₄)alkyl; —(C₂-C₆)alkenyl; —(C₁-C₃)alkylene-Y; —(C₂-C₃)alkenylene-Y; —(C₂-C₃)alkynylene-Y or —Y; and Y in R3 represents a monoradical coming from a cycle selected from a (C₃-C₆)cycloalkane, a heterocycle, benzene and a bicycle, wherein all these cycles can be optionally substituted as defined above.

In another embodiment in a compound of formula I or Ia, R2 represents —(CH₂)_(s)—N(COR3)-A-J-T; A represents —(C₁-C₄)alkylene-; —(C₁-C₄)alkylene-Z- or -Z-; Z in A represents a biradical coming from a cycle selected from a (C₃-C₆)cycloalkane, a heterocycle, benzene and a bicycle, wherein all these cycles can be optionally substituted with one or more substituents selected from the group —F, —Cl, —Br, —S(C₁-C₄)alkyl, —(C₁-C₄)alkyl optionally substituted by one or more —OH or —F and —O(C₁-C₄)alkyl optionally substituted by one or more —OH or —F; J represents a single bond; and T represents —H.

In another embodiment in a compound of formula I or Ia, R2 represents —(CH₂)_(s)—N(COR3)-A-J-T; A represents —(C₁-C₄)alkylene-; —(C₁-C₄)alkylene-Z- or -Z-; Z in A represents an unsubstituted biradical coming from a cycle selected from a (C₃-C₆)cycloalkane and benzene; J represents a single bond; and T represents —H.

In another embodiment in a compound of formula I or Ia, R2 represents —(CH₂)_(s)—N(R4)-B-J-T; R4 represents —(C₄-C₁₀)alkyl optionally substituted by one or more substituents selected from —F, —Cl, —Br and —O(C₁-C₄)alkyl; —(C₁-C₄)alkylene-Y; or —Y; and Y in R4 represents a monoradical coming from a cycle selected from a (C₃-C₆)cycloalkane, a heterocycle, benzene and a bicycle, wherein all these cycles can be optionally substituted as defined above.

In another embodiment in a compound of formula I or Ia, R2 represents —(CH₂)_(s)—N(R4)-B-J-T, B represents —(C₁-C₄)alkylene-Z- or -Z-; Z in B represents a biradical coming from a cycle selected from a (C₃-C₆)cycloalkane, a heterocycle, benzene and a bicycle, wherein all these cycles can be optionally substituted as defined above; J represents a single bond; and T represents —H.

Furthermore, all possible combinations of the above-mentioned embodiments form also part of this invention.

The compounds of the present invention may contain one or more basic nitrogen atoms and, therefore, they may form salts with acids, that also form part of this invention. Examples of pharmaceutically acceptable salts include, among others, addition salts with inorganic acids such as hydrochloric, hydrobromic, hydroiodic, nitric, perchloric, sulphuric and phosphoric acid, as well as addition salts of organic acids such as acetic, methanesulfonic, trifluoromethanesulfonic, ethanesulfonic, benzenesulfonic, p-toluenesulfonic, benzoic, camphorsulfonic, mandelic, oxalic, succinic, fumaric, tartaric, and maleic acid. Likewise, compounds of the present invention may contain one or more acid protons and, therefore, they may form salts with bases, that also form part of this invention. Examples of these salts include salts with metal cations, such as for example an alkaline metal ion, an alkaline-earth metal ion or an aluminium ion; or it may be coordinated with an organic with an organic or inorganic base. An acceptable organic base includes among others diethylamine and triethylamine. An acceptable inorganic base includes aluminium hydroxide, calcium hydroxide, potassium hydroxide, sodium carbonate, and sodium hydroxide. There may be more than one cation or anion depending on the number of functions with charge and on the valency of cations and anions.

Salts derived from pharmaceutically acceptable organic nontoxic bases include salts of primary, secondary, and tertiary amines, substituted amines including naturally occurring substituted amines, cyclic amines, and basic ion exchange resins, such as arginine, betaine, caffeine, choline, N,N-dibenzylethylenediamine, diethylamine, 2-diethylaminoethanol, 2-dimethylaminoethanol, ethanolamine, ethylenediamine, N-ethylmorpholine, ethylpiperidine, glucamine, glucosamine, histidine, hydrabamine, isopropylamine, lysine, methylglucamine, morpholine, piperazine, piperidine, polyamine resins, procaine, purines, theobromine, triethylamine, trimethylamine, tripropylamine, tromethamine, and the like.

There is no limitation on the type of salt that can be used provided that these are pharmaceutically acceptable when they are used for therapeutic purposes. Salts can be synthesized from the parent compound which contains a basic or acidic moiety by conventional chemical methods. Generally, such salts can be prepared by reacting the free acid or base forms of these compounds with a stoichiometric amount of the appropriate base or acid in water or in an organic solvent, such as ether, ethyl acetate, ethanol, isopropanol, or acetonitrile or in a mixture of the two. The compounds of formula I and their salts differ in some physical properties but they are equivalent for the purposes of the present invention.

Some of the compounds of formula I of the present invention may exist in unsolvated as well as solvated forms such as, for example, hydrates. The present invention encompasses all such above-mentioned forms which are pharmaceutically active.

Some of the compounds of general formula I may exhibit polymorphism, encompassing the present invention all the possible polymorphic forms, and mixtures thereof. Various polymorphs may be prepared by crystallization under different conditions or by heating or melting the compound followed by gradual or fast cooling. The presence of polymorphs may be determined by solid NMR spectroscopy, IR spectroscopy, differential scanning calorimetry, powder X-ray diffraction or such other techniques.

Compounds of formula I of the present invention comprise at least one chiral center. Additionally, compounds of formula I of the present invention may have further chiral centres. The present invention includes each one of the possible stereoisomers and mixtures thereof, particularly racemic mixtures thereof. A single enantiomer may be prepared by any of the commonly used processes, for example, by chromatographic separation of the racemic mixture on a stationary chiral phase, by resolution of the racemic mixture by fractional crystallisation techniques of the diastereomeric salts thereof, by chiral synthesis, by enzymatic resolution or by biotransformation. This resolution can be carried out on any chiral synthetic intermediate or on products of general Formula I. Alternatively, any enantiomer of a compound of the general Formula I may be obtained by enantiospecific synthesis using optically pure starting materials or reagents of known configuration.

Some of the compounds of the present invention may exist as several diastereoisomers, which may be separated by conventional techniques such as chromatography or fractional crystallization. Some compounds of the present invention may exhibit cis/trans isomers. The present invention includes each of the geometric isomers and its mixtures. The present invention covers all isomers and mixtures thereof (for example racemic mixtures) whether obtained by synthesis and also by physically mixing them.

The present invention relates to a process for the preparation of the above said novel compounds, their derivatives, their analogues, their tautomeric forms, their stereoisomers, their polymorphs or their pharmaceutical acceptable salts and solvates.

The compounds of the present invention may be synthesized using the methods described below, as well as other processes known in the field of organic synthesis. Preferred methods include, but are not limited to, the general processes shown in the attached schemes. Unless otherwise stated the groups R1, R2, R3, R4, R5, R6, s, A, B, J, and T have the meaning described in general formula I.

A compound of formula I may be obtained in general by hydrolysis of a compound of formula II, wherein R7 represents (C₁-C₄)alkyl. This reaction can be carried out in the presence of a base such as an alkaline hydroxide in a solvent such as tetrahydrofuran, aqueous methanol or a mixture thereof, at a temperature comprised between room temperature and the temperature of the boiling point of the solvent, preferably at room temperature.

A compound of formula II may be obtained as shown in the above scheme by Williamson ether synthesis (see for instance Bal-Tembe et al., Bioorg. Med. Chem. 1997, 5, 1381-1388; Cantello et al., J. Med. Chem. 1994, vol. 37, p. 3977-3985 or EP 875510) or by Mitsunobu conditions (Mitsunobu, Synthesis 1981, 1; Hughes, Org. React. 1992, 42, 335).

In the first case, phenol ester III may be reacted with R2-LG (IVa), wherein LG represents a leaving group, such as for instance a halogen including —Cl, —Br, —I or an alkylsulfonate or arylsulfonate, including mesylate, tosylate or nosylate. This reaction is carried out in the presence of a base, such as NaH, K₂CO₃ or Cs₂CO₃, in a solvent such as N,N-dimethylformamide, acetone or ethyl acetate, at a temperature comprised between room temperature and the temperature of the boiling point of the solvent, preferably heating.

In the second case, a compound of formula III may be reacted with an alcohol of formula R2-OH (IVb) using for example, diethyl azodicarboxylate (DEAD) and triphenylphosphine in tetrahydrofuran as a solvent, at a temperature comprised between room temperature and the temperature of the boiling point of the solvent, preferably at room temperature.

Isolated enantiomeric forms of formula Ia and Ib can be obtained either by chiral resolution of a compound of formula I or starting from the corresponding chiral compounds IIIa and IIIb respectively.

A compound of formula II wherein R2 represents —(CH₂)_(s)—N(COR3)-A-J-T (i.e. compound of formula IIa) may also be obtained by acylation of a compound of formula Va with a compound of formula R3-COX (VIa), wherein X represents halogen, preferably Cl.

This reaction is carried out in the presence of a base such as triethylamine, in a solvent such as dichloromethane or ethyl acetate, at a temperature comprised between room temperature and the temperature of the boiling point of the solvent.

Some compounds of formula IIa can also be obtained by reacting a compound Va with the corresponding acid of formula VIb (see for instance Elmore, Amino Acids Pep. Proteins 2001, 32, 107-162). This reaction is carried out in the presence of a coupling agent, such as the combination of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (EDC) and 1-hydroxybenzotriazol (HOBT) in the presence of a base such as triethylamine, in a solvent such as ethyl acetate or tetrahydrofuran, at a temperature comprised between room temperature and the temperature of the boiling point of the solvent.

Some compounds of formula II wherein R2 represents —(CH₂)_(s)—N(R4)-B-J-T (i.e. compounds of formula IIb) may also be obtained by reacting a compound of formula Vb with an alkylating agent of formula R4-LG (VII), wherein LG has the meaning previously described.

This reaction is carried out in the presence of a base, such as K₂CO₃, in a suitable solvent, such as N,N-dimethylformamide or acetonitrile, at a temperature and the temperature of the boiling point of the solvent, preferably room temperature.

Alternatively compounds of formula II can be obtained by solid synthesis using different types of polimeric solid resins, such as Wang or 2-chlorotrityl resins (Collins et al. J. Med. Chem. 1998, 41, 5037-5054). Compounds of formula III can be prepared following similar procedures to those described in Cobb et al., J. Med. Chem. 1998, 41, 5055-69.

Compounds IVa and IVb wherein R2 represents —(CH₂)_(s)—N(R4)-B-J-T (i.e. compounds of formula IVaa and IVba respectively) may be obtained as shown in the following scheme:

Compound VIII is acylated with a compound of formula IX to yield a compound of formula X, wherein R9 represents —CO₂(C₁-C₄)alkyl or —OCO(C₁-C₄)alkyl, under the same conditions as the reaction of compound Va with VIa to give compound IIa. Reduction of compound X with a reducing agent such as lithium aluminium hydride in diethyl ether affords compound IVba.

Alternatively, compound VIII can be reacted with an alkylating agent of formula XI to afford compound IVba (Daoud et al., J. Indian Chem. Soc. 1989, 66, 316-318). Compound of formula IVaa is obtained by converting the hydroxyl group of compound IVba into a leaving group. This reaction may be carried out using a sulfonyl halide such as methanesulfonyl chloride in the presence of a base, such as pyridine or triethylamine in a solvent such as dichloromethane or chloroform. Alternatively, compound IVba can be reacted with a halogenating agent such as SOCl₂ in a solvent such as tetrahydrofuran.

Compound VIII can be also converted directly into a compound of formula IVaa by reaction with a compound of formula XII, wherein each LG independently represents a leaving group as defined above, in the same conditions as described for the conversion of VIII into IVba.

A compound of formula V (including compounds of formula Va and Vb) may be obtained using two different synthetic sequences as shown in the following scheme:

Phenol III can be reacted with a protected amine of formula XIVa or XIVb, to yield a compound of formula XIII, wherein R8 represents -A-J-T or -B-J-T, LG represents a leaving group as previously described and PG represents a protecting group, such as for example, trifluoroacetyl or 2-nitrobenzenesulfonyl. The reaction is carried out under the same conditions described for the conversion of a compound of formula III into a compound of formula II. Compound V is subsequently obtained by deprotection of compound XIII. This reaction is carried out under different conditions depending upon the nature of the protecting group (see for instance Harland et al. Synthesis 1984, 941-43, Hirschmann et al. J. Amer. Chem. Soc. 1993, 12550-12568 for the group trifluororacetamide and Lin et al. Tetrahedron Letters 2000, 3309-3313 for the 2-nitrobenzenesulfonylamide group).

Alternatively a compound of formula V can be obtained by reacting phenol III with a secondary amine of formula XVa by Williamson ether synthesis. Compounds of formula VIII are commercially available or can be prepared by methods similar to those described for instance in WO 03/53966 or EP 875510. Compounds XIVa and XIVb can be obtained by reaction of the corresponding unprotected amine of formula XV and a protecting group (see Protective Groups in Organic Synthesis, John Wiley & Sons, 3rd Edition, 1999).

A compound of formula XV can be obtained using the following synthetic scheme:

Compound XVI is acylated to afford compound XVII under the same conditions for the reaction of compound Va and VIa to give compound IIa. Reduction of compound XVII gives compound XVb under the conditions described for the reduction of compound X. Compounds XVb wherein the amino group is less reactive than the hydroxyl group can be converted into compounds XVa under the conditions described for the conversion of IVba into IVaa.

Moreover, a compound of formula XVc can be obtained starting from a compound of formula XVIII.

This conversion can be carried out by reaction with an aldehyde of formula R10-CHO (XIX), wherein R10 represents R8 wherein the group attached to the N is —CH₂, in the presence of a reducing agent, such as triacetoxyborohydride or cyanoborohydride in a solvent such as 1,2-dichloroethane. Alternatively, compound XVIII can be reacted with compound XX or a derivative thereof to afford the corresponding amide as previously described. The reduction of the resulting product gives rise a compound of formula XVc. Compounds VIa, VIb, VII, IX, XI, XII, XVI, XVIII, XIX and XX are commercially available or can be easily obtained by conventional methods.

As it will be obvious to a person skilled in the art some of the reactions described above can also be carried out on compounds of formula I.

The compounds of the present invention are ligands of the PPARγ receptor. Therefore, they are expectedly useful for the treatment or prevention of a condition mediated by PPARγ in a subject in need thereof, including a human.

Thus, the present invention relates to the use of these compounds for the preparation of a medicament for the treatment or prevention of metabolic diseases, cardiovascular diseases associated with metabolic syndrome (including vascular restenosis), inflammatory diseases, cancer, bone diseases (particularly osteoporosis), skin wound healing, cutaneous disorders associated with an anomalous differentiation of epidermic cells, particularly the formation of keloids, and other disorders where insulin resistance is a component, including Syndrome X.

As an example, metabolic diseases that can be treated or prevented include non-insulin-dependent diabetes mellitus, obesity, hypercholesterolaemia (including raising HDL levels), dyslipidemia (including hyperlipidemia and hypertriglyceridemia), and other lipid-mediated pathologies.

As an example, inflammatory diseases that can be treated or prevented include rheumatoid arthritis, atherosclerosis, psoriasis, inflammatory bowel disease and pancreatitis.

The compounds described herein may be used to treat these diseases or conditions separately, or may be used to treat them concurrently with the treatment of obesity.

The present invention further provides for pharmaceutical compositions comprising a compound of formula I or a pharmaceutical salt or solvate thereof together with one or more pharmaceutically acceptable excipients, in either single or multiple doses. The examples of the excipients mentioned below are given by way of illustration only and are not to be construed as limiting the scope of the invention.

The compounds of the present invention can be administered in the form of any pharmaceutical formulation. The pharmaceutical formulation will depend upon the nature of the active compound and its route of administration. Any route of administration may be used, for example such as oral, buccal, pulmonary, topical, parenteral (including subcutaneous, intramuscular, and intravenous), transdermal, ocular (ophthalmic), inhalation, intranasal, otic, transmucosal, implant or rectal administration. However oral, topical or parenteral administration are preferred.

Solid compositions for oral administration include among others tablets, granulates and hard gelatin capsules, formulated both as immediate release or modified release formulations.

The manufacturing method may be based on a simple mixture, dry granulation, wet granulation or lyophilization of the active compound with excipients. These excipients may be binding agents, such as syrup, acacia, gelatin, sorbitol, gum tragacanth, corn starch or polyvinylpyrrolidone; fillers such as lactose, sugar, microcrystalline cellulose, maize-starch, calcium phosphate or sorbitol; lubricants such as magnesium stearate, stearic acid, talc, polyethylene glycol or silica; disintegrants such as potato starch, alginic acid or sodium starch glycollate; wetting agents, such as sodium lauryl sulfate, sweetening agents such as sucrose, lactose, dextrose, mannitol, sorbitol or saccharin; bioadhesive agents such as hydroxypropyl cellulose, poly(vinyl alcohol), poly(isobutylene), sodium carboxymethyl cellulose; glidants such as magnesium trisilicate, powdered cellulose, starch, talc or tribasic calcium phosphate; flow enhancers such as colloidal silicon dioxide; release modifiers such as xanthan gum, ethylcellulose, carbomer, hydroxypropyl methyl cellulose or wax or osmotic agents such as potassium bicarbonate or sodium chloride.

The tablets may be coated according to methods well-known in the art such as aqueous dispersion coating, solvent-based coating or drying coating.

The active compound can also be incorporated by coating onto inert pellets using film-coating agents, by extrusion and spheronization process, by hot melting pelletization or it can be in the form of a troche or lozenge. When a dosage unit form is a capsule, it may contain, in addition to materials of the above type, a liquid carrier such as a fatty oil or wax.

Powders and granulates for the preparation of oral suspensions by the addition of water can be obtained by mixing the active compound with dispersing or wetting agents; suspending agents, anticaking agents, buffering agents and preservatives. Other excipients may also be added, for example sweetening, flavouring and colouring agents.

Alternatively, the compounds of the present invention may be incorporated into oral liquid preparations such as emulsions, solutions, dispersions, suspensions, syrups, elixirs or in the form of soft gelatin capsules. They may contain commonly-used inert diluents, such as purified water, ethanol, sorbitol, glycerol, polyethylene glycols (macrogols) and propylene glycol. Aid compositions can also contain coadjuvants such as wetting, suspending, sweetening, flavouring agents, preservatives, buffers, chelating agents and antioxidants.

Solutions or suspensions may be prepared in water suitably mixed with a surfactant such as sodium lauryl sulfate. Dispersions may also be prepared in glycerol, liquid polyethylene glycols and mixtures thereof in oils. Under ordinary conditions of storage and use, these preparations contain a preservative to prevent the growth of microorganisms. Moreover, formulations containing these compounds may be presented as a dry product constitution with water or other suitable vehicle before use.

Injectable preparations for parenteral administration comprise sterile solutions, suspensions or emulsions in oily or aqueous vehicles, and may contain coadjuvants, such as suspending, stabilizing, tonicity agents or dispersing agents.

For nasal administration, the preparation may contain a compound of formula I dissolved or suspended in a liquid carrier, in particular an aqueous carrier, for aerosol application. The carrier may contain additives such as solubilizing agents, e.g. propylene glycol, surfactants, absorption enhancers such as lecithin (phosphatidylcholine) or cyclodextrin, or preservatives such as parabenes.

The compound can also be formulated for its topical application. Formulations include creams, lotions, gels, powders, solutions, shampoo preparations, oral paste, mouth wash preparations and patches wherein the compound is dispersed or dissolved in suitable excipients. These excipients may be antimicrobial preservatives such as imidurea, propylparaben, propylene glycol or methylparaben; emulsifying agents such as cetyl alcohol, methylcellulose, poloxamer or medium-chain triglycerides; emulsion stabilizers such as glyceril monostearate, magnesium aluminium silicate, cyclodextrins or wax; humectants such as triacetin, glycerin, propylene glycol or sorbitol; penetrants enhancing agents such as isopropyl miristate; buffering agents such as malic acid, potassium citrate or sodium phosphate dibasic; surfactants such as docusate sodium, sodium lauryl sulfate, polysorbates or sorbitan esters; thickening agents such as hydroxyethyl cellulose, hydroxypropyl cellulose or polyethylene oxide.

The effective dosage of active ingredient may vary depending on the particular compound administered, the route of administration, the nature and severity of the disease to be treated, as well as the age, the general condition and body weight of the patient, among other factors. A representative example of a suitable dosage range is from about 0.001 to about 100 mg/Kg body weight per day, which can be administered as a single or divided doses. However, the dosage administered will be generally left to the discretion of the physician.

PPARγ2 Binding Assay

The cDNA encoding for the open reading frame of the hPPARγ2 was amplified by PCR (polymerase chain reaction) and inserted in the plasmid pGEX-4T-2. This construction (pGEX-hPPARγ) was introduced into E. coli where it was overexpressed and semipurified as a fusion protein with glutathione S-transferase (GST) (Elbrecht et al., J. Biol. Chem. 1999, 274, 7913-7922).

The binding of the compounds to the GST-hPPARγ2 s was determined by modifications in the method described by Lehmann et al. (J. Biol. Chem. 1995, 270, 12953-12957). The receptors (2.5 μg) were incubated in 96-well plates in the presence or in the absence of the products with [³H]BRL-49853 (100 nM) for 3 h at 4° C., in a final volume of 200 μL of buffer Tris-HCl 10 mM pH: 8.0, containing KCl 50 mM and DTT 10 mM. Non-specific binding was determined in the presence of BRL-49853 100 μM. The reaction mixture was transferred to a Multiscreen Durapore (Millipore) microplate containing glutathione-Sepharose 4B in every well. The reaction mixture was left to incubate with the resin during 10 min, and then centrifuged at 735 g during 2 min. To dissociate the receptor bound to the resin, reduced glutathione 10 mM is added and incubated during 10 min. The receptor was eluted by centrifugation. Then, scintillation liquid was added to the elution and the contained radioactivity was quantified by liquid scintillation spectroscopy (Microbeta Wallac, Perkin Elmer).

LBD-hPPARs Transactivation Assay

COS-7 cells were cultivated in 24-well plates and transfected with the pFACMV plasmids that encode the chimeric proteins containing the GAL4 DNA binding domain fused to the PPARγ LBD. The reporter plasmid for the foregoing constructions was pFR-Luc, which contains five repetitions of the GAL4-response element in front of a promoter that controls the transcription of the luciferase gene. Lipofectamine was used as a transfection agent.

The plasmids of the chimeric receptors and the reporter gene were inserted in the cells by transitory transfection in COS-7 cells in culture. When the products were added to the culture for 48 h, the luciferase activity showed the effect of the PPAR activity modulation on the transcription of the reporter construction (Wright et al., J. Biol. Chem. 2000, 275, 1873).

Cloning of Human PPARγ2

The human PPAR cDNA was amplified through RT-PCR. For hPPARγ2, RNA was obtained from human white adipose tissue. Each amplified fragment was cloned into pBluescript (Stratagene®) and sequenced. One clone for each construction was selected and used as template for further subcloning and PCR amplifications.

GST-Fused Protein Construction

To generate this chimeric protein, the complete cDNA of the human PPAR was cloned into pGEX4T2 (Amersham Biosciences). The fragment was obtained from the pBluescript-cDNAs clones digested with endonucleases. To assess the plasmid identity and to ensure the in-phase cloning of the proteins, pGEX construction was sequenced. GST-hPPARγ2 fusion protein was generated in Escherichia coli (BL21 strain DE3). Cells were cultured in LB medium to a density of A600=1.6 odu, and induced for overexpression by addition of isopropyl-1-thio-β-D-galactopyranoside (IPTG)-induced cultures to a final concentration of 0.5 mM. The IPTG-induced cultures were grown at room temperature o/n, before cells were harvested by centrifugation at 5000 g for 15 min. After sonication, the GST-fusion protein was purified from the cell pellet using glutathione-Sepharose beads, following the procedure recommended by the manufacturer (Amersham Pharmacia Biotech). Excess of gluthatione was removed o/n by dyalisis at 4° C. Receptor purity was visualized by SDS-PAGE and protein content was determined by Bradford method. Receptor aliquots were stored at −80° C. until use.

In Table 1, affinity and functional activity data of some of the compounds of the present invention are shown.

TABLE 1 Example Affinity Functional activity Number PPARγ⁽¹⁾ PPARγ I_121 ++ ANTAGONIST I_128 ++ — I_149 + — I_178 +++ — I_198 ++ PARTIAL AGONIST I_262 +++ AGONIST I_265 +++ AGONIST I_280 +++ — I_303 +++ — I_375 +++ PARTIAL AGONIST I_379 ++ — I_391 ++ — I_410 +++ ANTAGONIST I_412 +++ — I_418 ++ PARTIAL AGONIST I_438 ++ — I_440 ++ — I_467 +++ — I_469 ++ — ⁽¹⁾+++: Ki <500 nM, ++: 500 nM < Ki < 1500 nM, +: Ki >1500 nM

Additional objects, advantages and novel features of the invention will be set forth in part in the description, and in part will become apparent to those skilled in the art upon examination of the description or may be learned by practice of the invention. The present invention will be further illustrated by the following examples. The examples are given by way of illustration only and are not to be construed as limiting the scope of the invention.

The nomenclature of the different compounds used in the present document is based on the software AUTONOM (Automatic Nomenclature) from the Beilstein Institute, which uses the IUPAC systematic nomenclature.

LC-MS spectra have been performed using the following chromatographic equipment: Hewlett-Packard model 1100, equipped with a selective mass detector model 1100 VL, autosampler, ChemStation software and a laser printer (mass spectrometry ionization mode: Atmospheric pressure ionisation with positive ion detection) and using the following chromatographic methods:

Method A: Column Kromasil 100 C18, 40×4.0 mm, 3.5 μm, flow: 0.7 mL/min, eluent: A=0.1% formic acid in water, B=0.1% formic acid in acetonitrile, gradient: 0 min 5% B-8 min 90% B.

Method B: Column: Gemini 5u C18 110, 40×4.0 mm, flow: 0.7 mL/min, eluent: A=0.1% formic acid in water, B=0.1% formic acid in acetonitrile, gradient: 0 min 5% B-8 min 90% B.

¹H-NMR spectra of the compounds have been recorded using a VARIAN GEMINI-200 MHz and a VARIAN UNITY-300 MHz equipment and chemical shifts are expressed as ppm (δ) from the internal reference TMS. Mass spectra have been obtained with an Agilent 1100 VL mass spectrometer.

The following abbreviations have been used in the examples:

DEAD: diethyl azodicarboxylate

DMF: N,N-dimethylformamide

EDC: 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide eq: molar equivalent EtOAc: ethyl acetate HOBT: 1-hydroxybenzotriazol LC-MS: liquid chromatography-mass spectrometry rt: retention time THF: tetrahydrofuran TMS: trimethylsylane

Intermediates IIIa and IIIb:

Compounds of formula IIIa and IIIb can be prepared following similar procedures to those described in Cobb et al., J. Med. Chem. 1998, 41, 5055-69.

IIIa_(—)1: (S)-2-(2-Benzoylphenylamino)-3-(4-hydroxyphenyl)propionic acid methyl ester; rt: 7.357, MS [M+1]⁺: 376.

IIIb_(—)1: (R)-2-(2-Benzoylphenylamino)-3-(4-hydroxyphenyl)propionic acid methyl ester; rt: 7.357, MS [M+1]⁺: 376.

Intermediates XIII:

Compounds of formula XIII shown in Table 2 were obtained starting from a phenol III and an amine derivative of formula XIVa or XIVb following one of the procedures A-D described below.

PROCEDURE A: A 0.5 M suspension of phenol III (1 eq) in EtOAc containing anhydrous potassium carbonate (3 eq) and compound XIVa (1.3 eq) was refluxed for 18 h. Then, the suspension was allowed to cool down and the white solid was filtered. The solvent was distilled off under reduced pressure, and the obtained residue was purified by column chromatography.

PROCEDURE B: A 0.5 M suspension of phenol III (1 eq) in anhydrous DMF containing cesium carbonate (3 eq), compound XIVa (1.3 eq) and potassium iodide (catalythic amount) was heated at 80° C. for 18 h. Then, the suspension was allowed to cool down at room temperature, and treated with water and EtOAc. The organic layer was washed three times with brine, dried over anhydrous sodium sulfate and filtered. The solvent was distilled off under reduced pressure, and the obtained residue was purified by column chromatography.

PROCEDURE C: To a 0.1 M solution of phenol III (1 eq) in anhydrous DMF, containing a catalythic amount of potassium iodide, sodium hydride (60%, 1.1 eq) was added. The resulting suspension was stirred at room temperature for 1 hour and then compound XIVa (1.1 eq) was added. The reaction mixture was stirred at 80° C. for 18 h, and then allowed to cool down to room temperature. After treating with water and EtOAc, the organic layer was washed three times with brine, dried over anhydrous sodium sulfate and filtered. The solvent was distilled off under reduced pressure, and the obtained residue was purified by column chromatography.

PROCEDURE D: To a 0.2 M solution of phenol III (1 eq) in THF, containing compound XIVb (2.2 eq) and triphenylphosphine (2.2 eq), DEAD (2.2 eq) was added under inert atmosphere. The solution was stirred at room temperature for 18 h. Then, the solvent was distilled off under reduced pressure, and the obtained residue was purified by column chromatography.

TABLE 2 Example Starting HPLC Number product Compound name ¹H-NMR/LC-MS Method XIII_1 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4-{2- 8.86 (d, 1H), A [benzyl-(2,2,2-trifluoroacetyl)amino]- 7.62-7.56 (ca, 2H), ethoxy}phenyl)propionic acid methyl 7.56-7.16 (ca, ester 12H), 6.79 (d, 2H), 6.68-6.55 (ca, 2H), 4.80 (s, 2H), 4.40 (q, 1H), 4.10 (t, 2H), 3.75-3.60 (ca, 5H), 3.19 (dd, 1H), 3.09 (dd, 1H) XIII_2 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4-{3- rt: 9.383 A [benzyl-(2,2,2-trifluoroacetyl)amino]- MS [M + 1]⁺: 619 propoxy}phenyl)propionic acid methyl ester XIII_3 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4-{2- rt: 9.706 A [cyclohexyl-(2,2,2-trifluoroacetyl)- MS [M + 1]⁺: 597 amino]ethoxy}phenyl)propionic acid methyl ester XIII_4 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4-{2- rt: 9.287 A [tert-butyl-(2,2,2-trifluoroacetyl)amino]- MS [M + 1]⁺: 571 ethoxy}phenyl)propionic acid methyl ester XIII_5 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4-{2- rt: 8.969 A [cyclopropylmethyl(2- MS [M + 1]⁺: 658 nitrobenzenesulfonyl)amino]ethoxy}- phenyl)propionic acid methyl ester XIII_6 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4-{3- rt: 9.103 A [cyclopropylmethyl(2- MS [M + 1]⁺: 672 nitrobenzenesulfonyl)amino]propoxy}- phenyl)propionic acid methyl ester XIII_7 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4-{2- rt: 9.323 A [(3-methylbenzyl)(2- MS [M + 1]⁺: _(—) nitrobenzenesulfonyl)amino]ethoxy}- phenyl)propionic acid methyl ester XIII_8 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4-{3- rt: 9.449 A [(3-methylbenzyl)(2- MS [M + 1]⁺: _(—) nitrobenzenesulfonyl)amino]propoxy}- phenyl)propionic acid methyl ester XIII_9 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4-{2- rt: 8.948 A [(2-nitrobenzenesulfonyl)propylamino]- MS [M + 1]⁺: 646 ethoxy}phenyl)propionic acid methyl ester XIII_10 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4-{2- rt: 8.726 A [ethyl-(2-nitrobenzenesulfonyl)amino]- MS [M + 1]⁺: 632 ethoxy}phenyl)propionic acid methyl ester

Intermediates V:

Compounds of formula V shown in Table 3 were obtained starting from phenol III and an amine derivative of formula XVa following one of the procedures A-C described above or alternatively starting from compound XIII using procedures E-F described below.

PROCEDURE E: To a 0.1 M solution of compound XIII (1 eq) (PG=trifluoroacetyl) in a mixture of THF:methanol (3:1), a 1 M aqueous solution of lithium hydroxide (5 eq) was added. The solution was stirred for 18 h at room temperature, then diluted with a mixture of water/EtOAc, and then acidified to pH=5 with HCl 1 N. The organic layer was dried over anhydrous sodium sulfate and filtered. The solvent was distilled off under reduced pressure, and the obtained residue was redissolved in methanol to afford a 0.1 M solution, which was treated with thionyl chloride (3.2 eq). The solution was refluxed for 18 h, and then allowed to cool down to room temperature. The solvent was distilled off under reduced pressure. The obtained residue was purified by column chromatography.

PROCEDURE F: To a 0.1 M solution of compound XIII (PG=2-nitrobenzenesulfonyl, 1 eq) in DMF containing thiophenol (1 eq), KO^(t)Bu (2 eq) was added. The solution was stirred at room temperature for 6 h and then diluted with a mixture of water/EtOAc. The organic layer was washed three times with brine, dried over anhydrous sodium sulfate and filtered. The solvent was distilled off under reduced pressure, and the obtained residue was purified by column chromatography.

TABLE 3 Example Starting HPLC Number product Compound name ¹H-NMR/LC-MS Method V_1 XIII_1 (S)-2-(2-Benzoylphenylamino)-3-[4- 8.86 (d, 1H), A (2-benzylaminoethoxy)phenyl]- 7.62-7.56 (ca, 2H), propionic acid methyl ester 7.56-7.40 (ca, 6H), 7.40-7.27 (ca, 4H), 7.14 (d, 2H), 6.83 (d, 2H), 6.65-6.53 (ca, 2H), 4.63 (q, 1H), 4.13 (t, 2H), 3.99 (s, 2H), 3.68 (s, 3H), 3.19 (dd, 1H), 3.09 (dd, 1H), 3.03 (t, 2H) V_2 XIII_2 (S)-2-(2-Benzoylphenylamino)-3-[4- rt: 6.385 A (3-benzylaminopropoxy)phenyl]- MS [M + 1]⁺: 523 propionic acid methyl ester V_3 XIII_3 (S)-2-(2-Benzoylphenylamino)-3-[4- rt: 6.495 A (2-cyclohexylaminoethoxy)phenyl]- MS [M + 1]⁺: 501 propionic acid methyl ester V_4 XIII_4 (S)-2-(2-Benzoylphenylamino)-3-[4- rt: 6.209 A (2-tert-butylaminoethoxy)phenyl]- MS [M + 1]⁺: 475 propionic acid methyl ester V_5 XIII_5 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 5.882 A [2-(cyclopropylmethylamino)ethoxy]- MS [M + 1]⁺: 473 phenyl}propionic acid methyl ester V_6 XIII_6 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 6.354 A [3-(cyclopropylmethylamino)- MS [M + 1]⁺: 487 propoxy]phenyl}propionic acid methyl ester V_7 XIII_7 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 6.591 A [2-(3-methylbenzylamino)ethoxy]- MS [M + 1]⁺: 523 phenyl}propionic acid methyl ester V_8 XIII_8 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 6.758 A [3-(3-methylbenzylamino)propoxy]- MS [M + 1]⁺: 537 phenyl}propionic acid methyl ester V_9 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-[4- rt: 8.96 A (2-phenylaminoethoxy)phenyl]- MS [M + 1]⁺: 495 propionic acid methyl ester V_10 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-[4- rt: 8.993 A (3-phenylaminopropoxy)phenyl]- MS [M + 1]⁺: 509 propionic acid methyl ester V_11 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.131 A [2-(2-fluorophenylamino)ethoxy]- MS [M + 1]⁺: 513 phenyl}propionic acid methyl ester V_12 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.013 A [2-(3-fluorophenylamino)ethoxy]- MS [M + 1]⁺: 513 phenyl}propionic acid methyl ester V_13 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.876 A [2-(4-fluorophenylamino)ethoxy]- MS [M + 1]⁺: 513 phenyl}propionic acid methyl ester V_14 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-[4- rt: 9.247 A (2-o-tolylaminoethoxy)phenyl]- MS [M + 1]⁺: 509 propionic acid methyl ester V_15 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-[4- rt: 9.127 A (2-m-tolylaminoethoxy)phenyl]- MS [M + 1]⁺: 509 propionic acid methyl ester V_16 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-[4- rt: 9.014 A (2-p-tolylaminoethoxy)phenyl]- MS [M + 1]⁺: 509 propionic acid methyl ester V_17 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.431 A [2-(2-chlorophenylamino)ethoxy]- MS [M, M + 2]⁺: 530, phenyl}propionic acid methyl ester 532 V_18 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.293 A [2-(3-chlorophenylamino)ethoxy]- MS [M, M + 2]⁺: 530, phenyl}propionic acid methyl ester 532 V_19 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.265 A [2-(4-chlorophenylamino)ethoxy]- MS [M, M + 2]⁺: 530, phenyl}propionic acid methyl ester 532 V_20 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-[4- rt: 9.377 A (3-o-tolylaminopropoxy)phenyl]- MS [M + 1]⁺: 523 propionic acid methyl ester V_21 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-[4- rt: 9.11 A (3-m-tolylaminopropoxy)phenyl]- MS [M + 1]⁺: 523 propionic acid methyl ester V_22 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-[4- rt: 8.714 A (3-p-tolylaminopropoxy)phenyl]- MS [M + 1]⁺: 523 propionic acid methyl ester V_23 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.632 A [3-(2-chlorophenylamino)propoxy]- MS [M, M + 2]⁺: 543, phenyl}propionic acid methyl ester 545 V_24 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.474 A [3-(3-chlorophenylamino)propoxy]- MS [M, M + 2]⁺: 543, phenyl}propionic acid methyl ester 545 V_25 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.435 A [3-(4-chlorophenylamino)propoxy]- MS [M, M + 2]⁺: 543, phenyl}propionic acid methyl ester 545 V_26 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.202 A [2-(naphthalen-1-ylamino)ethoxy]- MS [M + 1]⁺: 545 phenyl}propionic acid methyl ester V_27 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.189 A [2-(3-methylsulfanylphenylamino)- MS [M + 1]⁺: 541 ethoxy]phenyl}propionic acid methyl ester V_28 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.178 A [2-(4-methylsulfanylphenylamino)- MS [M + 1]⁺: 541 ethoxy]phenyl}propionic acid methyl ester V_29 IIIb_1 (R)-2-(2-Benzoylphenylamino)-3-[4- rt: 8.968 A (2-phenylaminoethoxy)phenyl]- MS [M + 1]⁺: 495 propionic acid methyl ester V_30 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.417 A [2-(naphthalen-2-ylamino)ethoxy]- MS [M + 1]⁺: 545 phenyl}propionic acid methyl ester V_31 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.369 A [3-(2-fluorophenylamino)propoxy]- MS [M + 1]⁺: 527 phenyl}propionic acid methyl ester V_32 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.233 A [3-(3-fluorophenylamino)propoxy]- MS [M + 1]⁺: 527 phenyl}propionic acid methyl ester V_33 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.992 A [3-(4-fluorophenylamino)propoxy]- MS [M + 1]⁺: 527 phenyl}propionic acid methyl ester V_34 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.085 A [2-(2-methoxyphenylamino)ethoxy]- MS [M + 1]⁺: 525 phenyl}propionic acid methyl ester V_35 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.850 A [2-(3-methoxyphenylamino)ethoxy]- MS [M + 1]⁺: 525 phenyl}propionic acid methyl ester V_36 XIII_10 (S)-2-(2-Benzoylphenylamino)-3-[4- rt: 5.889 A (2-ethylaminoethoxy)phenyl]- MS [M + 1]⁺: 447 propionic acid methyl ester V_37 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.097 A [3-(2-methoxyphenylamino)propoxy]- MS [M + 1]⁺: 539 phenyl}propionic acid methyl ester V_38 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.923 A [3-(3-methoxyphenylamino)propoxy]- MS [M + 1]⁺: 539 phenyl}propionic acid methyl ester V_39 XIII_9 (S)-2-(2-Benzoylphenylamino)-3-[4- rt: 6.063 A (2-propylaminoethoxy)phenyl]- MS [M + 1]⁺: 461 propionic acid methyl ester

Intermediates II:

Compounds of formula II shown in Table 4 were obtained starting from phenol III and a compound of formula IVa or IVb following one of the procedures A-D described above.

TABLE 4 Example Starting HPLC Number product Compound name ¹H-NMR/LC-MS Method II_1 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.561 A [2-(benzylindan-5-ylamino)ethoxy]- MS [M + 1]⁺: 625 phenyl}propionic acid methyl ester II_2 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.023 A {2-[benzyl(2,6-difluorophenyl)amino]- MS [M + 1]⁺: 621 ethoxy}phenyl)propionic acid methyl ester II_3 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.22 A {2-[(2-chlorophenyl)-(2-fluorobenzyl)- MS [M + 1]⁺: 638 amino]ethoxy}phenyl)propionic acid methyl ester II_4 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.977 A {2-[benzyl-(2-fluorophenyl)amino]- MS [M + 1]⁺: 603 ethoxy}phenyl)propionic acid methyl ester II_5 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.123 A {2-[(2-methylbenzyl)phenylamino]- MS [M + 1]⁺: 599 ethoxy}phenyl)propionic acid methyl ester II_6 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.204 A {2-[(3-chlorophenyl)-(2- MS [M + 1]⁺: 650 methoxybenzyl)amino]ethoxy}- phenyl)propionic acid methyl ester II_7 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.134 A {2-[(2-methoxybenzyl)-m-tolylamino]- MS [M + 1]⁺: 629 ethoxy}phenyl)propionic acid methyl ester II_8 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.014 A {3-[(2-methoxybenzyl)phenylamino]- MS [M + 1]⁺: 629 propoxy}phenyl)propionic acid methyl ester II_9 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.25 A [2-(benzyl-o-tolylamino)ethoxy]- MS [M + 1]⁺: 599 phenyl}propionic acid methyl ester II_10 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.356 A {2-[benzyl-(3-ethylphenyl)amino]- MS [M + 1]⁺: 613 ethoxy}phenyl)propionic acid methyl ester II_11 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.864 A {2-[benzyl-(3-fluorophenyl)amino]- MS [M + 1]⁺: 603 ethoxy}phenyl)propionic acid methyl ester II_12 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.119 A {2-[(2-chlorophenyl)-(3- MS [M + 1]⁺: 650 methoxybenzyl)amino]ethoxy}- phenyl)propionic acid methyl ester II_13 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.012 A {2-[(3-chlorophenyl)-(3- MS [M + 1]⁺: 650 methoxybenzyl)amino]ethoxy}- phenyl)propionic acid methyl ester II_14 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.004 A {2-[(3-methoxybenzyl)-m-tolylamino]- MS [M + 1]⁺: 629 ethoxy}phenyl)propionic acid methyl ester II_15 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.931 A {3-[(3-methoxybenzyl)phenylamino]- MS [M + 1]⁺: 629 propoxy}phenyl)propionic acid methyl ester II_16 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.127 A [2-(benzyl-m-tolylamino)ethoxy]- MS [M + 1]⁺: 599 phenyl}propionic acid methyl ester II_17 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.164 A {2-[benzyl-(4-chlorophenyl)amino]- MS [M + 1]⁺: 619 ethoxy}phenyl)propionic acid methyl ester II_18 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.863 A {2-[benzyl-(4-fluorophenyl)amino]- MS [M + 1]⁺: 603 ethoxy}phenyl)propionic acid methyl ester II_19 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.172 A {2-[(4-methylbenzyl)phenylamino]- MS [M + 1]⁺: 599 ethoxy}phenyl)propionic acid methyl ester II_20 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.879 A {3-[(4-methoxybenzyl)phenylamino]- MS [M + 1]⁺: 629 propoxy}phenyl)propionic acid methyl ester II_21 IIIa_1 (S)-2-(Benzoylphenylamino)-3-{4-[2- rt: 10.592 A (di-p-tolylamino)ethoxy]phenyl}- MS [M + 1]⁺: 599 propionic acid methyl ester II_22 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.174 A [2-(benzyl-p-tolylamino)ethoxy]- MS [M + 1]⁺: 599 phenyl}propionic acid methyl ester II_23 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.601 A [3-(benzylindan-5-ylamino)propoxy]- MS [M + 1]⁺: 639 phenyl}propionic acid methyl ester II_24 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.507 A {3-[benzyl-(3-ethylphenyl)amino]- MS [M + 1]⁺: 627 propoxy}phenyl)propionic acid methyl ester II_25 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.261 A [3-(benzyl-m-tolylamino)propoxy]- MS [M + 1]⁺: 613 phenyl}propionic acid methyl ester II_26 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.27 A [3-(benzyl-p-tolylamino)propoxy]- MS [M + 1]⁺: 613 phenyl}propionic acid methyl ester II_27 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 7.251 A [3-(benzylcyclohexylamino)propoxy]- MS [M + 1]⁺: 605 phenyl}propionic acid methyl ester II_28 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- 8.92 (d, 1H), 7.60 (d, A [3-(benzylphenylamino)propoxy]- 2H), 7.60-7.15 (ca, phenyl}propionic acid methyl ester 17H), 6.85-6.55 (ca, 4H), 4.55 (s, 2H), 4.39 (q, 1H), 3.97 (t, 2H), 3.69 (s, 3H), 3.62 (t, 2H), 3.22 (dd, 1H), 3.13 (dd, 1H), 2.20-2.00 (ca, 2H) II_29 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.281 A {2-[(2-fluorophenyl)isobutylamino]- MS [M + 1]⁺: 569 ethoxy}phenyl)propionic acid methyl ester II_30 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.614 A [2-(isobutyl-o-tolylamino)ethoxy]- MS [M + 1]⁺: 565 phenyl}propionic acid methyl ester II_31 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.455 A [3-(isobutyl-o-tolylamino)propoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid methyl ester II_32 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.109 A {2-[(3-fluorophenyl)isobutylamino]- MS [M + 1]⁺: 569 ethoxy}phenyl)propionic acid methyl ester II_33 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.397 A {2-[isobutyl-m-tolylamino]ethoxy}- MS [M + 1]⁺: 565 phenyl)propionic acid methyl ester II_34 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.412 A [3-(isobutyl-m-tolylamino)propoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid methyl ester II_35 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 7.539 A [2-(benzylphenethylamino)ethoxy]- MS [M + 1]⁺: 613 phenyl}propionic acid methyl ester II_36 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.223 A [2-(cyclobutylmethyl-o-tolylamino)- MS [M + 1]⁺: 577 ethoxy]phenyl}propionic acid methyl ester II_37 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 7.03 A [2-(benzylcyclopentylamino)ethoxy]- MS [M + 1]⁺: 577 phenyl}propionic acid methyl ester II_38 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 7.811 A [3-(cyclopentylphenylamino)- MS [M + 1]⁺: 577 propoxy]phenyl}propionic acid methyl ester II_39 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.786 A {2-[cyclopentylmethyl-(2- MS [M + 1]⁺: 595 fluorophenyl)amino]ethoxy}phenyl)- propionic acid methyl ester II_40 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.602 A [2-(cyclopentymethylphenylamino)- MS [M + 1]⁺: 577 ethoxy]phenyl}propionic acid methyl ester II_41 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 6.954 A [2-(benzylcyclopropylmethylamino)- MS [M + 1]⁺: 563 ethoxy]phenyl}propionic acid methyl ester II_42 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 7.052 A [3-(benzylcyclopropylmethylamino)- MS [M + 1]⁺: 577 propoxy]phenyl}propionic acid methyl ester II_43 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.936 A {2-[(2-methoxybenzyl)phenylamino]- MS [M + 1]⁺: 615 ethoxy}phenyl)propionic acid methyl ester II_44 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.8 A {2-[(3-methoxybenzyl)phenylamino]- MS [M + 1]⁺: 615 ethoxy}phenyl)propionic acid methyl ester II_45 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.831 A {2-[(3-methoxyphenyl)phenylamino]- MS [M + 1]⁺: 601 ethoxy}phenyl)propionic acid methyl ester II_46 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.788 A {2-[(4-methoxybenzyl)phenylamino]- MS [M + 1]⁺: 615 ethoxy}phenyl)propionic acid methyl ester II_47 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: — A {2-[(4-tert-butylbenzyl)phenylamino]- MS [M + 1]⁺: 641 ethoxy}phenyl)propionic acid methyl ester II_48 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- 8.89 (d, 1H), 7.59 (d, A [2-(benzylphenylamino)ethoxy]- 2H), 7.55-7.40 (ca, phenyl}propionic acid methyl ester 4H), 7.40-7.15 (ca, 11H), 6.85-6.55 (ca, 8H), 4.67 (s, 2H), 4.42 (m, 1H), 4.18 (t, 2H), 3.85 (t, 2H), 3.71 (s, 3H), 3.30-3.10 (ca, 2H) II_49 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.206 A [2-(cyclobutylmethylphenylamino)- MS [M + 1]⁺: 563 ethoxy]phenyl}propionic acid methyl ester II_50 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.01 A [2-(cyclohexylphenylamino)ethoxy]- MS [M + 1]⁺: 577 phenyl}propionic acid methyl ester II_51 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: — A [2-(cyclohexylmethylphenylamino)- MS [M + 1]⁺: 589 ethoxy]phenyl}propionic acid methyl ester II_52 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.769 A [2-(cyclopentylphenylamino)ethoxy]- MS [M + 1]⁺: 563 phenyl}propionic acid methyl ester II_53 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.696 A [2-(cyclopropylmethylphenylamino)- MS [M + 1]⁺: 549 ethoxy]phenyl}propionic acid methyl ester II_54 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- 8.98 (d, 1H), A [2-(diphenylamino)ethoxy]phenyl}- 7.70-7.60 (ca, 2H), propionic acid methyl ester 7.60-7.45 (ca, 3H), 7.45-7.15 (ca, 8H), 7.15-6.95 (ca, 6H), 6.85 (d, 2H), 6.75-6.60 (ca, 2H), 4.44 (q, 1H), 4.17 (s, 4H), 3.72 (s, 3H), 3.30-3.10 (ca, 2H). II_55 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: _(—) A {2-[cyclohexylmethyl-(2- MS [M + 1]⁺: _(—) fluorophenyl)amino]ethoxy}phenyl)- propionic acid methyl ester II_56 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: _(—) A {2-[(3-chlorophenyl)- MS [M + 1]⁺: _(—) cyclopentylmethylamino]ethoxy}- phenyl)propionic acid methyl ester II_57 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.527 A {3-[cyclobutylmethyl-(3- MS [M + 1]⁺: 595 fluorophenyl)amino]propoxy}phenyl)- propionic acid methyl ester II_58 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.994 A [3-(cyclobutylmethyl-m-tolylamino)- MS [M + 1]⁺: 591 propoxy]phenyl}propionic acid methyl ester II_59 IIIb_1 (R)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.945 A [2-(benzylphenylamino)ethoxy]- MS [M + 1]⁺: 585 phenyl}propionic acid methyl ester II_60 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: _(—) A {2-[(2-chlorophenyl)- MS [M + 1]⁺: _(—) cyclopentylmethylamino]ethoxy}- phenyl)propionic acid methyl ester II_61 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.831 A {2-[(2-fluorophenyl)thiophen-2- MS [M + 1]⁺: 609 ylmethylamino]ethoxy}phenyl)- propionic acid methyl ester II_62 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.561 A {3-[(2-fluorophenyl)isobutylamino]- MS [M + 1]⁺: 583 propoxy}phenyl)propionic acid methyl ester II_63 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: _(—) A {3-[cyclopentylmethyl-(2- MS [M + 1]⁺: _(—) fluorophenyl)amino]propoxy}phenyl)- propionic acid methyl ester II_64 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.655 A [3-(cyclobutylmethyl-o-tolylamino)- MS [M + 1]⁺: 591 propoxy]phenyl}propionic acid methyl ester II_65 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.752 A {2-[(3-fluorophenyl)thiophen-2- MS [M + 1]⁺: 609 ylmethylamino]ethoxy}phenyl)- propionic acid methyl ester II_66 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.996 A [2-(thiophen-2-ylmethyl-m- MS [M + 1]⁺: 605 tolylamino)ethoxy]phenyl}propionic acid methyl ester II_67 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.131 A [3-(thiophen-3-ylmethyl-m- MS [M + 1]⁺: 316 tolylamino)propoxy]phenyl}propionic acid methyl ester II_68 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.929 A [3-(furan-2-ylmethyl-m-tolylamino)- MS [M + 1]⁺: 603 propoxy]phenyl}propionic acid methyl ester II_69 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.744 A {2-[(4-fluorophenyl)thiophen-2- MS [M + 1]⁺: 609 ylmethylamino]ethoxy}phenyl)- propionic acid methyl ester II_70 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.795 A [2-(phenylthiophen-2- MS [M + 1]⁺: 591 ylmethylamino)ethoxy]phenyl}- propionic acid methyl ester II_71 IIIa_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.933 A [3-(phenylthiophen-2- MS [M + 1]⁺: 605 ylmethylamino)propoxy]phenyl}- propionic acid methyl ester

Intermediates IIa:

Compounds of formula IIa shown in Table 5 were obtained starting from a compound Va and a compound of formula VIa or VIb, following one of the procedures G-H described below.

PROCEDURE G: To a 0.2 M solution of compound Va (1 eq) in dichloromethane or EtOAc, triethylamine (3 eq) and a solution of an acyl chloride VIa (1.2 eq) were added. After stirring for 18 h, the crude was treated with 5% NaHCO₃. The organic layer was washed twice with 5% NaHCO₃ and once with brine. The organic layer was dried over anhydrous sodium sulfate and filtered. The solvent was distilled off under reduced pressure. The obtained residue was purified by column chromatography.

PROCEDURE H: To a 0.3 M suspension of compound Va (1 eq) in EtOAc containing HOBT (1.5 eq) and EDC (1.5 eq), triethylamine (3 eq) was added. Then, carboxylic acid VIb (1 eq) was added and stirred for 18 h. The reaction mixture was treated with water, the organic layer was separated and the aqueous layer was extracted once with EtOAc. The combined organic layers were washed once with 5% NaHCO₃ and once with brine, dried over anhydrous sodium sulfate, and filtered. The solvent was distilled off under reduced pressure, and the obtained residue was purified by column chromatography.

TABLE 5 Example Starting HPLC Number product Compound name ¹H-NMR/LC-MS Method IIa_1 V_17 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.069 A {2-[(2-chlorophenyl)-(2- MS [M + 1]⁺: 597 methylacryloyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_2 V_23 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.926 B {3-[(2-chlorophenyl)-(2- MS [M, M + 2]⁺: 611, methylacryloyl)amino]propoxy}- 613 phenyl)propionic acid methyl ester IIa_3 V_17 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.034 A {2-[but-2-(E)-enoyl-(2-chlorophenyl)- MS [M, M + 2]⁺: 597, amino]ethoxy}phenyl)propionic acid 599 methyl ester IIa_4 V_17 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.532 A {2-[(2-chlorophenyl)-(3- MS [M, M + 2]⁺: 613, methylbutyryl)amino]ethoxy}phenyl)- 615 propionic acid methyl ester IIa_5 V_17 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.427 A {2-[(2-chlorophenyl)- MS [M, M + 2]⁺: 611, cyclobutanecarbonylamino]ethoxy}- 613 phenyl)propionic acid methyl ester IIa_6 V_17 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.657 A {2-[(2-chlorophenyl)- MS [M, M + 2]⁺: 625, cyclopentanecarbonylamino]ethoxy}- 627 phenyl)propionic acid methyl ester IIa_7 V_17 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.094 A {2-[(2-chlorophenyl)- MS [M, M + 2]⁺: 597, cyclopropanecarbonylamino]ethoxy}- 599 phenyl)propionic acid methyl ester IIa_8 V_23 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.28 A {3-[(2-chlorophenyl)- MS [M, M + 2]⁺: 611, cyclopropanecarbonylamino]- 613 propoxy}phenyl)propionic acid methyl ester IIa_9 V_17 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.049 A {2-[(2-chlorophenyl)propionylamino]- MS [M, M + 2]⁺: 585, ethoxy}phenyl)propionic acid methyl 587 ester IIa_10 V_23 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.247 A {3-[(2-chlorophenyl)propionylamino]- MS [M, M + 2]⁺: 599, propoxy}phenyl)propionic acid 601 methyl ester IIa_11 V_17 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.28 A {2-[(2-chlorophenyl)isobutyrylamino]- MS [M, M + 2]⁺: 599, ethoxy}phenyl)propionic acid methyl 601 ester IIa_12 V_23 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.126 B {3-[(2-chlorophenyl)isobutyrylamino]- MS [M, M + 2]⁺: 613, propoxy}phenyl)propionic acid 615 methyl ester IIa_13 V_17 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.069 A {2-[butyryl-(2-chlorophenyl)amino]- MS [M, M + 2]⁺: 597, ethoxy}phenyl)propionic acid methyl 599 ester IIa_14 V_23 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.148 B {3-[butyryl-(2-chlorophenyl)amino]- MS [M, M + 2]⁺: 613, propoxy}phenyl)propionic acid 615 methyl ester IIa_15 V_23 (S)-3-(4-{3-[Acryloyl-(2- rt: 9.102 A chlorophenyl)amino]propoxy}- MS [M, M + 2]⁺: 597, phenyl)-2-(2-benzoylphenylamino)- 599 propionic acid methyl ester IIa_16 V_11 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.961 A {2-[(2-fluorophenyl)-(thiophene-2- MS [M + 1]⁺: 623 carbonyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_17 V_11 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.857 A {2-[(2-fluorophenyl)-(2- MS [M + 1]⁺: 581 methylacryloyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_18 V_11 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.282 A {2-[(2-fluorophenyl)-(3- MS [M + 1]⁺: 597 methylbutyryl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_19 V_11 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.185 A {2-[cyclobutanecarbonyl-(2- MS [M + 1]⁺: 595 fluorophenyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_20 V_11 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.412 A {2-[cyclopentanecarbonyl-(2- MS [M + 1]⁺: 609 fluorophenyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_21 V_11 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.865 A {2-[cyclopropanecarbonyl-(2- MS [M + 1]⁺: 581 fluorophenyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_22 V_11 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.796 A {2-[(2-fluorophenyl)propionylamino]- MS [M + 1]⁺: 569 ethoxy}phenyl)propionic acid methyl ester IIa_23 V_11 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.04 A {2-[(2-fluorophenyl)isobutyrylamino]- MS [M + 1]⁺: 583 ethoxy}phenyl)propionic acid methyl ester IIa_24 V_11 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.05 A {2-[butyryl-(2-fluorophenyl)amino]- MS [M + 1]⁺: 583 ethoxy}phenyl)propionic acid methyl ester IIa_25 V_11 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.408 A {2-[(2,2-dimethylpropionyl)-(2- MS [M + 1]⁺: 597 fluorophenyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_26 V_20 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.828 B {3-[(2-methylacryloyl)-o-tolylamino]- MS [M + 1]⁺: 591 propoxy}phenyl)propionic acid methyl ester IIa_27 V_14 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.684 A {2-[(2-ethylbutyryl)-o-tolylamino]- MS [M + 1]⁺: 607 ethoxy}phenyl)propionic acid methyl ester IIa_28 V_20 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.165 B {3-[(3-methylbut-2-(E)-enoyl)-o- MS [M + 1]⁺: 605 tolylamino]propoxy}phenyl)propionic acid methyl ester IIa_29 V_20 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.911 B [3-(but-2-(E)-enoyl-o-tolylamino)- MS [M + 1]⁺: 591 propoxy]phenyl}propionic acid methyl ester IIa_30 V_14 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.788 A {2-[(3,3-dimethylbutyryl)-o- MS [M + 1]⁺: 607 tolylamino]ethoxy}phenyl)propionic acid methyl ester IIa_31 V_14 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.465 A {2-[(3-methylbutyryl)-o-tolylamino]- MS [M + 1]⁺: 593 ethoxy}phenyl)propionic acid methyl ester IIa_32 V_20 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.331 B {3-[(3-methylbutyryl)-o-tolylamino]- MS [M + 1]⁺: 607 propoxy}phenyl)propionic acid methyl ester IIa_33 V_20 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.129 B [3-(o-tolylpent-4-enoylamino)- MS [M + 1]⁺: 605 propoxy]phenyl}propionic acid methyl ester IIa_34 V_14 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.378 A [2-(cyclobutanecarbonyl-o- MS [M + 1]⁺: 591 tolylamino)ethoxy]phenyl}propionic acid methyl ester IIa_35 V_14 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.607 A [2-(cyclopentanecarbonyl-o- MS [M + 1]⁺: 605 tolylamino)ethoxy]phenyl}propionic acid methyl ester IIa_36 V_20 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.849 B [3-(propionyl-o-tolylamino)propoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid methyl ester IIa_37 V_14 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.22 A [2-(isobutyryl-o-tolylamino)ethoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid methyl ester IIa_38 V_20 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.08 B [3-(isobutyryl-o-tolylamino)propoxy]- MS [M + 1]⁺: 593 phenyl}propionic acid methyl ester IIa_39 V_20 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.348 B [3-(pentanoyl-o-tolylamino)propoxy]- MS [M + 1]⁺: 607 phenyl}propionic acid methyl ester IIa_40 V_14 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.233 A [2-(butyryl-o-tolylamino)ethoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid methyl ester IIa_41 V_20 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.094 B [3-(butyryl-o-tolylamino)propoxy]- MS [M + 1]⁺: 593 phenyl}propionic acid methyl ester IIa_42 V_14 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.077 A [2-(benzoyl-o-tolylamino)ethoxy]- MS [M + 1]⁺: 613 phenyl}propionic acid methyl ester IIa_43 V_14 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.597 A {2-[(2,2-dimethylpropionyl)-o- MS [M + 1]⁺: 593 tolylamino]ethoxy}phenyl)propionic acid methyl ester IIa_44 V_20 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.435 B {3-[(2,2-dimethylpropionyl)-o- MS [M + 1]⁺: 607 tolylamino]propoxy}phenyl)propionic acid methyl ester IIa_45 V_20 (S)-3-{4-[3-(Acryloyl-o-tolylamino)- rt: 9.781 B propoxy]phenyl}-2-(2- MS [M + 1]⁺: 577 benzoylphenylamino)propionic acid methyl ester IIa_46 V_18 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.126 A {2-[(3-chlorophenyl)-(2- MS [M, M + 2]⁺: 597, methylacryloyl)amino]ethoxy}- 599 phenyl)propionic acid methyl ester IIa_47 V_18 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.184 A {2-[but-2-(E)-enoyl-(3-chlorophenyl)- MS [M, M + 2]⁺: 597, amino]ethoxy]phenyl}propionic acid 599 methyl ester IIa_48 V_24 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.348 A {3-[but-2-(E)-enoyl-(3-chlorophenyl)- MS [M, M + 2]⁺: 611, amino]propoxy}phenyl)propionic acid 613 methyl ester IIa_49 V_18 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.557 A {2-[(3-chlorophenyl)-(3- MS [M, M + 2]⁺: 613, methylbutyryl)amino]ethoxy}phenyl)- 615 propionic acid methyl ester IIa_50 V_18 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.375 A {2-[(3-chlorophenyl)-pent-4- MS [M, M + 2]⁺: 611, enoylamino]ethoxy}phenyl)propionic 613 acid methyl ester IIa_51 V_18 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.488 A {2-[(3-chlorophenyl)- MS [M, M + 2]⁺: 611, cyclobutanecarbonylamino]ethoxy}- 613 phenyl)propionic acid methyl ester IIa_52 V_18 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.708 A {2-[(3-chlorophenyl)- MS [M, M + 2]⁺: 625, cyclopentanecarbonylamino]ethoxy}- 627 phenyl)propionic acid methyl ester IIa_53 V_18 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.217 A {2-[(3-chlorophenyl)- MS [M, M + 2]⁺: 597, cyclopropanecarbonylamino]ethoxy}- 599 phenyl)propionic acid methyl ester IIa_54 V_24 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.401 A {3-[(3-chlorophenyl)- MS [M, M + 2]⁺: 611, cyclopropanecarbonylamino]- 613 propoxy}phenyl)propionic acid methyl ester IIa_55 V_18 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.097 A {2-[(3-chlorophenyl)propionylamino]- MS [M, M + 2]⁺: 585, ethoxy}phenyl)propionic acid methyl 587 ester IIa_56 V_24 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.279 A {3-[(3-chlorophenyl)propionylamino]- MS [M, M + 2]⁺: 599, propoxy}phenyl)propionic acid 601 methyl ester IIa_57 V_18 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.332 A {2-[(3-chlorophenyl)isobutyrylamino]- MS [M, M + 2]⁺: 599, ethoxy}phenyl)propionic acid methyl 601 ester IIa_58 V_24 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.502 A {3-[(3-chlorophenyl)isobutyrylamino]- MS [M, M + 2]⁺: 613, propoxy}phenyl)propionic acid 615 methyl ester IIa_59 V_18 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.339 A {2-[butyryl-(3-chlorophenyl)amino]- MS [M, M + 2]⁺: 599, ethoxy}phenyl)propionic acid methyl 601 ester IIa_60 V_24 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.508 A {3-[butyryl-(3-chlorophenyl)amino]- MS [M, M + 2]⁺: 613, propoxy}phenyl)propionic acid 615 methyl ester IIa_61 V_18 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.669 A {2-[(3-chlorophenyl)-(2,2- MS [M, M + 2]⁺: 613, dimethylpropionyl)amino]ethoxy}- 615 phenyl)propionic acid methyl ester IIa_62 V_24 (S)-3-(4-{3-[Acryloyl-(3- rt: 9.202 A chlorophenyl)amino]propoxy}- MS [M, M + 2]⁺: 597, phenyl)-2-(2-benzoylphenylamino)- 599 propionic acid methyl ester IIa_63 V_12 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.016 A {2-[(3-fluorophenyl)-(thiophene-2- MS [M + 1]⁺: 623 carbonyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_64 V_12 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.86 A {2-[(3-fluorophenyl)-(2- MS [M + 1]⁺: 581 methylacryloyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_65 V_12 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.284 A {2-[(3-fluorophenyl)-(3- MS [M + 1]⁺: 597 methylbutyryl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_66 V_12 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.198 A {2-[cyclobutanecarbonyl-(3- MS [M + 1]⁺: 595 fluorophenyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_67 V_12 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.424 A {2-[cyclopentanecarbonyl-(3- MS [M + 1]⁺: 609 fluorophenyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_68 V_12 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.93 A {2-[cyclopropanecarbonyl-(3- MS [M + 1]⁺: 581 fluorophenyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_69 V_12 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.805 A {2-[(3-fluorophenyl)propionylamino]- MS [M + 1]⁺: 569 ethoxy}phenyl)propionic acid methyl ester IIa_70 V_12 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.047 A {2-[(3-fluorophenyl)isobutyrylamino]- MS [M + 1]⁺: 583 ethoxy}phenyl)propionic acid methyl ester IIa_71 V_12 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.057 A {2-[butyryl-(3-fluorophenyl)amino]- MS [M + 1]⁺: 583 ethoxy}phenyl)propionic acid methyl ester IIa_72 V_12 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.393 A {2-[(2,2-dimethylpropionyl)-(3- MS [M + 1]⁺: 597 fluorophenyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_73 V_8 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.199 A {3-[(2-methylacryloyl)-(3- MS [M + 1]⁺: 605 methylbenzyl)amino]propoxy}- phenyl)propionic acid methyl ester IIa_74 V_7 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.678 A {2-[(2-ethylbutyryl)-(3-methylbenzyl)- MS [M + 1]⁺: 621 amino]ethoxy}phenyl)propionic acid methyl ester IIa_75 V_8 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.382 A {3-[(3-methylbenzyl)-(3-methylbut-2- MS [M + 1]⁺: 619 (E)-enoyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_76 V_8 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.153 A {3-[but-2-(E)-enoyl-(3-methylbenzyl)- MS [M + 1]⁺: 605 amino]propoxy}phenyl)propionic acid methyl ester IIa_77 V_7 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.728 A {2-[(3,3-dimethylbutyryl)-(3- MS [M + 1]⁺: 621 methylbenzyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_78 V_7 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.471 A {2-[(3-methylbenzyl)-(3- MS [M + 1]⁺: 607 methylbutyryl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_79 V_8 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.549 A {3-[(3-methylbenzyl)-(3- MS [M + 1]⁺: 621 methylbutyryl)amino]propoxy}- phenyl)propionic acid methyl ester IIa_80 V_7 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.389 A {2-[cyclobutanecarbonyl-(3- MS [M + 1]⁺: 605 methylbenzyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_81 V_8 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.464 A {3-[cyclobutanecarbonyl-(3- MS [M + 1]⁺: 619 methylbenzyl)amino]propoxy}- phenyl)propionic acid methyl ester IIa_82 V_7 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.588 A {2-[cyclopentanecarbonyl-(3- MS [M + 1]⁺: 619 methylbenzyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_83 V_8 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.194 A {3-[cyclopropanecarbonyl-(3- MS [M + 1]⁺: 605 methylbenzyl)amino]propoxy}- phenyl)propionic acid methyl ester IIa_84 V_8 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.095 A {3-[(3-methylbenzyl)propionylamino]- MS [M + 1]⁺: 593 propoxy}phenyl)propionic acid methyl ester IIa_85 V_7 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.23 A {2-[isobutyryl-(3-methylbenzyl)- MS [M + 1]⁺: 593 amino]ethoxy}phenyl)propionic acid methyl ester IIa_86 V_8 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.319 A {3-[isobutyryl-(3-methylbenzyl)- MS [M + 1]⁺: 607 amino]propoxy}phenyl)propionic acid methyl ester IIa_87 V_7 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.247 A {2-[butyryl-(3-methylbenzyl)amino]- MS [M + 1]⁺: 593 ethoxy}phenyl)propionic acid methyl ester IIa_88 V_8 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.328 A {3-[butyryl-(3-methylbenzyl)amino]- MS [M + 1]⁺: 607 propoxy}phenyl)propionic acid methyl ester IIa_89 V_7 (S)-3-(4-{2-[Benzoyl-(3- rt: 9.28 A methylbenzyl)amino]ethoxy}phenyl)- MS [M + 1]⁺: 627 2-(2-benzoylphenylamino)propionic acid methyl ester IIa_90 V_7 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.602 A {2-[(2,2-dimethylpropionyl)-(3- MS [M + 1]⁺: 607 methylbenzyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_91 V_8 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.635 A {3-[(2,2-dimethylpropionyl)-(3- MS [M + 1]⁺: 621 methylbenzyl)amino]propoxy}- phenyl)propionic acid methyl ester IIa_92 V_21 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.906 B {3-[(2-methylacryloyl)-m-tolylamino]- MS [M + 1]⁺: 591 propoxy}phenyl)propionic acid methyl ester IIa_93 V_15 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.75 A {2-[(2-ethylbutyryl)-m-tolylamino]- MS [M + 1]⁺: 607 ethoxy}phenyl)propionic acid methyl ester IIa_94 V_21 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.231 B {3-[(3-methylbut-2-(E)-enoyl)-m- MS [M + 1]⁺: 605 tolylamino]propoxy}phenyl)propionic acid methyl ester IIa_95 V_21 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.985 B [3-(but-2-(E)-enoyl-m-tolylamino)- MS [M + 1]⁺: 591 propoxy]phenyl}propionic acid methyl ester IIa_96 V_15 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.826 A {2-[(3,3-dimethylbutyryl)-m- MS [M + 1]⁺: 607 tolylamino]ethoxy}phenyl)propionic acid methyl ester IIa_97 V_15 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.518 A {2-[(3-methylbutyryl)-m-tolylamino]- MS [M + 1]⁺: 593 ethoxy}phenyl)propionic acid methyl ester IIa_98 V_15 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.46 A [2-(cyclobutanecarbonyl-m- MS [M + 1]⁺: 591 tolylamino)ethoxy]phenyl}propionic acid methyl ester IIa_99 V_15 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.671 A [2-(cyclopentanecarbonyl-m- MS [M + 1]⁺: 605 tolylamino)ethoxy]phenyl}propionic acid methyl ester IIa_100 V_21 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.041 B [3-(cyclopropanecarbonyl-m- MS [M + 1]⁺: 591 tolylamino)propoxy]phenyl}propionic acid methyl ester IIa_101 V_21 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.915 B [3-(propionyl-m-tolylamino)propoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid methyl ester IIa_102 V_15 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.287 A [2-(isobutyryl-m-tolylamino)ethoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid methyl ester IIa_103 V_21 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.134 B [3-(isobutyryl-m-tolylamino)propoxy]- MS [M + 1]⁺: 593 phenyl}propionic acid methyl ester IIa_104 V_21 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.398 B [3-(pentanoyl-m-tolylamino)propoxy]- MS [M + 1]⁺: 607 phenyl}propionic acid methyl ester IIa_105 V_15 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.296 A [2-(butyryl-m-tolylamino)ethoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid methyl ester IIa_106 V_21 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.146 B [3-(butyryl-m-tolylamino)propoxy]- MS [M + 1]⁺: 593 phenyl}propionic acid methyl ester IIa_107 V_15 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.176 A [2-(benzoyl-m-tolylamino)ethoxy]- MS [M + 1]⁺: 613 phenyl}propionic acid methyl ester IIa_108 V_15 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.659 A {2-[(2,2-dimethylpropionyl)-m- MS [M + 1]⁺: 593 tolylamino]ethoxy}phenyl)propionic acid methyl ester IIa_109 V_21 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.508 B {3-[(2,2-dimethylpropionyl)-m- MS [M + 1]⁺: 607 tolylamino]propoxy}phenyl)propionic acid methyl ester IIa_110 V_21 (S)-3-{4-[3-(Acryloyl-m-tolylamino)- rt: 9.85 B propoxy]phenyl}-2-(2- MS [M + 1]⁺: 577 benzoylphenylamino)propionic acid methyl ester IIa_111 V_19 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.173 A {2-[(4-chlorophenyl)-(2- MS [M, M + 2]⁺: 597, methylacryloyl)amino]ethoxy}- 599 phenyl)propionic acid methyl ester IIa_112 V_19 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.242 A {2-[but-2-(E)-enoyl-(4-chlorophenyl)- MS [M, M + 2]⁺: 597, amino]ethoxy}phenyl)propionic acid 599 methyl ester IIa_113 V_19 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.615 A {2-[(4-chlorophenyl)-(3- MS [M, M + 2]⁺: 613, methylbutyryl)amino]ethoxy}phenyl)- 615 propionic acid methyl ester IIa_114 V_19 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.428 A {2-[(4-chlorophenyl)-pent-4- MS [M, M + 2]⁺: 611, enoylamino]ethoxy}phenyl)propionic 613 acid methyl ester IIa_115 V_19 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.532 A {2-[(4-chlorophenyl)- MS [M, M + 2]⁺: 611, cyclobutanecarbonylamino]ethoxy}- 613 phenyl)propionic acid methyl ester IIa_116 V_19 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.763 A {2-[(4-chlorophenyl)- MS [M, M + 2]⁺: 625, cyclopentanecarbonylamino]ethoxy}- 627 phenyl)propionic acid methyl ester IIa_117 V_19 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.263 A {2-[(4-chlorophenyl)- MS [M, M + 2]⁺: 597, cyclopropanecarbonylamino]ethoxy}- 599 phenyl)propionic acid methyl ester IIa_118 V_25 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.442 A {3-[(4-chlorophenyl)- MS [M, M + 2]⁺: 611, cyclopropanecarbonylamino]- 613 propoxy}phenyl)propionic acid methyl ester IIa_119 V_19 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.146 A {2-[(4-chlorophenyl)propionylamino]- MS [M, M + 2]⁺: 585, ethoxy}phenyl)propionic acid methyl 587 ester IIa_120 V_25 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.323 A {3-[(4-chlorophenyl)propionylamino]- MS [M, M + 2]⁺: 599, propoxy}phenyl)propionic acid 601 methyl ester IIa_121 V_19 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.393 A {2-[(4-chlorophenyl)isobutyrylamino]- MS [M, M + 2]⁺: 599, ethoxy}phenyl)propionic acid methyl 601 ester IIa_122 V_25 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.558 A {3-[(4-chlorophenyl)isobutyrylamino]- MS [M, M + 2]⁺: 613, propoxy}phenyl)propionic acid 615 methyl ester IIa_123 V_19 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.393 A {2-[butyryl-(4-chlorophenyl)amino]- MS [M, M + 2]⁺: 599, ethoxy}phenyl)propionic acid methyl 601 ester IIa_124 V_25 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.558 A {3-[butyryl-(4-chlorophenyl)amino]- MS [M, M + 2]⁺: 613, propoxy}phenyl)propionic acid 615 methyl ester IIa_125 V_19 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.71 A {2-[(4-chlorophenyl)-(2,2- MS [M, M + 2]⁺: 613, dimethylpropionyl)amino]ethoxy}- 615 phenyl)propionic acid methyl ester IIa_126 V_25 (S)-3-(4-{3-[Acryloyl-(4- rt: 9.246 A chlorophenyl)amino]propoxy}- MS [M, M + 2]⁺: 597, phenyl)-2-(2-benzoylphenylamino)- 599 propionic acid methyl ester IIa_127 V_13 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.015 A {2-[(4-fluorophenyl)-(thiophene-2- MS [M + 1]⁺: 623 carbonyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_128 V_13 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.828 A {2-[(4-fluorophenyl)-(2- MS [M + 1]⁺: 581 methylacryloyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_129 V_13 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.141 A {2-[(4-fluorophenyl)-(3-methylbut-2- MS [M + 1]⁺: 595 (E)-enoyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_130 V_13 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.278 A {2-[(4-fluorophenyl)-(3- MS [M + 1]⁺: 597 methylbutyryl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_131 V_13 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.184 A {2-[cyclobutanecarbonyl-(4- MS [M + 1]⁺: 595 fluorophenyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_132 V_13 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.413 A {2-[cyclopentanecarbonyl-(4- MS [M + 1]⁺: 609 fluorophenyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_133 V_13 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.913 A {2-[cyclopropanecarbonyl-(4- MS [M + 1]⁺: 581 fluorophenyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_134 V_13 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.794 A {2-[(4-fluorophenyl)propionylamino]- MS [M + 1]⁺: 569 ethoxy}phenyl)propionic acid methyl ester IIa_135 V_13 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.038 A {2-[(4-fluorophenyl)isobutyrylamino]- MS [M + 1]⁺: 583 ethoxy}phenyl)propionic acid methyl ester IIa_136 V_13 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.046 A {2-[butyryl-(4-fluorophenyl)amino]- MS [M + 1]⁺: 583 ethoxy}phenyl)propionic acid methyl ester IIa_137 V_13 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.384 A {2-[(2,2-dimethylpropionyl)-(4- MS [M + 1]⁺: 597 fluorophenyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_138 V_22 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.202 A {3-[(2-methylacryloyl)-p-tolylamino]- MS [M + 1]⁺: 591 propoxy}phenyl)propionic acid methyl ester IIa_139 V_16 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.775 A {2-[(2-ethylbutyryl)-p-tolylamino]- MS [M + 1]⁺: 607 ethoxy}phenyl)propionic acid methyl ester IIa_140 V_16 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.851 A {2-[(3,3-dimethylbutyryl)-p- MS [M + 1]⁺: 607 tolylamino]ethoxy}phenyl)propionic acid methyl ester IIa_141 V_16 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.541 A {2-[(3-methylbutyryl)-p-tolylamino]- MS [M + 1]⁺: 593 ethoxy}phenyl)propionic acid methyl ester IIa_142 V_22 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.674 A {3-[(3-methylbutyryl)-p-tolylamino]- MS [M + 1]⁺: 607 propoxy}phenyl)propionic acid methyl ester IIa_143 V_16 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.472 A [2-(cyclobutanecarbonyl-p- MS [M + 1]⁺: 591 tolylamino)ethoxy]phenyl}propionic acid methyl ester IIa_144 V_22 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.605 A [3-(cyclobutanecarbonyl-p- MS [M + 1]⁺: 605 tolylamino)propoxy]phenyl}propionic acid methyl ester IIa_145 V_16 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.693 A [2-(cyclopentanecarbonyl-p- MS [M + 1]⁺: 605 tolylamino)ethoxy]phenyl}propionic acid methyl ester IIa_146 V_22 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.208 A [3-(propionyl-p-tolylamino)propoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid methyl ester IIa_147 V_16 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.307 A [2-(isobutyryl-p-tolylamino)ethoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid methyl ester IIa_148 V_22 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.443 A [3-(isobutyryl-p-tolylamino)propoxy]- MS [M + 1]⁺: 593 phenyl}propionic acid methyl ester IIa_149 V_16 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.313 A [2-(butyryl-p-tolylamino)ethoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid methyl ester IIa_150 V_16 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.169 A [2-(benzoyl-p-tolylamino)ethoxy]- MS [M + 1]⁺: 613 phenyl}propionic acid methyl ester IIa_151 V_16 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.671 A {2-[(2,2-dimethylpropionyl)-p- MS [M + 1]⁺: 593 tolylamino]ethoxy}phenyl)propionic acid methyl ester IIa_152 V_22 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.772 A {3-[(2,2-dimethylpropionyl)-p- MS [M + 1]⁺: 607 tolylamino]propoxy}phenyl)propionic acid methyl ester IIa_153 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.4 A {2-[benzyl(naphthalene-1-carbonyl)- MS [M + 1]⁺: 663 amino]ethoxy}phenyl)propionic acid methyl ester IIa_154 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.42 A {2-[benzyl(naphthalene-2-carbonyl)- MS [M + 1]⁺: 663 amino]ethoxy}phenyl)propionic acid methyl ester IIa_155 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.532 A {2-[benzyl(pyrazine-2-carbonyl)- MS [M + 1]⁺: 615 amino]ethoxy}phenyl)propionic acid methyl ester IIa_156 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.642 A {3-[benzyl(pyrazine-2-carbonyl)- MS [M + 1]⁺: 629 amino]propoxy}phenyl)propionic acid methyl ester IIa_157 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.693 A {2-[benzyl(pyridine-2-carbonyl)- MS [M + 1]⁺: 614 amino]ethoxy}phenyl)propionic acid methyl ester IIa_158 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.90 (d, 1H), 8.55, A {3-[benzyl(pyridine-2-carbonyl)- 8.45 (2 × d, 1H, amino]propoxy}phenyl)propionic acid rotamers mixture), methyl ester 7.77-7.12 (ca, 17H), 6.81-6.55 (ca, 4H), 4.80, 4.69 (2 × s, 2H, rotamers mixture), 4.39 (q, 1H), 3.39, 3.76 (2 × t, 2H, rotamers mixture), 3.70, 3.69 (2 × s, 3H, rotamers mixture), 3.62, 3.58 (2 × t, 2H, rotamers mixture), 3.20 (dd, 1H), 3.10 (m, 1H), 2.15-1.97 (ca, 2H) IIa_159 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.294 A {2-[benzyl(quinoline-2-carbonyl)- MS [M + 1]⁺: 664 amino]ethoxy}phenyl)propionic acid methyl ester IIa_160 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.90 (t, 1H), 8.21, A {3-[benzyl(quinoline-2-carbonyl)- 8.13 (2 × d, 1H, rotamers amino]propoxy}phenyl)propionic acid mixture), 8.04, methyl ester 7.80 (2 × t, 2H, rotamers mixture), 7.73-7.25 (ca, 14H), 7.18, 7.06 (2 × d, 2H, rotamers mixture), 6.82, 6.47 (2 × d, 2H, rotamers mixture), 6.70-6.55 (ca, 2H), 4.86, 4.79 (2 × s, 2H, rotamers mixture), 4.37 (q, 1H), 4.02, 3.77 (2 × t, 2H, rotamers mixture), 3.69-3.64 (ca, 5H), 3.25-3.05 (ca, 2H), 2.20-2.04 (ca, 2H) IIa_161 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.119 A {2-[benzyl(quinoxaline-2-carbonyl)- MS [M + 1]⁺: 665 amino]ethoxy}phenyl)propionic acid methyl ester IIa_162 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.211 A {3-[benzyl(quinoxaline-2-carbonyl)- MS [M + 1]⁺: 679 amino]propoxy}phenyl)propionic acid methyl ester IIa_163 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.07 A {2-[benzyl(thiophene-2-carbonyl)- MS [M + 1]⁺: 619 amino]ethoxy}phenyl)propionic acid methyl ester IIa_164 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.193 A {3-[benzyl(thiophene-2-carbonyl)- MS [M + 1]⁺: 633 amino]propoxy}phenyl)propionic acid methyl ester IIa_165 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.815 A {2-[benzyl(furan-3-carbonyl)amino]- MS [M + 1]⁺: 603 ethoxy}phenyl)propionic acid methyl ester IIa_166 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.907 A {3-[benzyl(furan-3-carbonyl)amino]- MS [M + 1]⁺: 617 propoxy}phenyl)propionic acid methyl ester IIa_167 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.1 A {2-[benzyl(isoquinoline-3-carbonyl)- MS [M + 1]⁺: 664 amino]ethoxy}phenyl)propionic acid methyl ester IIa_168 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- 9.19, 9.10 (2 × s, 1H, A {3-[benzyl(isoquinoline-3-carbonyl)- rotamers mixture), amino]propoxy}phenyl)propionic acid 8.90 (t, 1H), 8.07, methyl ester 7.99 (2 × s, 1H, rotamers mixture), 7.64-7.25 (ca, 16H), 7.18, 7.05 (2 × d, 2H, rotamers mixture), 6.82, 6.50 (2 × d, 2H, rotamers mixture), 6.65-6.55 (ca, 2H), 4.86, 4.76 (2 × s, 2H, rotamers mixture), 4.37 (m, 1H), 4.02, 3.77 (2 × t, 2H, rotamers mixture), 3.69-3.60 (ca, 5H), 3.25-3.05 (ca, 2H), 2.20-2.04 (ca, 2H) IIa_169 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.90 (d, 1H), A {2-[benzyl(pyridine-3-carbonyl)- 8.78-8.62 (ca, 2H), 7.83-7.73 (m amino]ethoxy}phenyl)propionic acid 1H), 7.59 (d, 2H), methyl ester 7.51-7.41 (ca, 4H), 7.37-7.20 (m, 9H), 6.85-6.72 (ca, 2H), 6.65-6.56 (ca, 2H), 4.87, 4.69 (2 × s, 2H, rotamers mixture), 4.40 (q, 1H), 4.25-3.58 (ca, 7H), 3.25 (dd, 1H), 3.10 (dd, 1H) IIa_170 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.90 (d, 1H), A {3-[benzyl(pyridine-3-carbonyl)- 8.67-8.59 (ca, 2H), 7.67-7.10 (m amino]propoxy}phenyl)propionic acid 16H), 6.81-6.55 (ca, methyl ester 4H), 4.80, 4.51 (2 × s, 2H, rotamers mixture), 4.39 (q, 1H), 4.02-3.39 (ca, 7H), 3.25 (dd, 1H), 3.10 (dd, 1H), 1.92-1.71 (ca, 2H) IIa_171 V_1 (S)-2-(2-Benzoylphenylamino)-3-{4- 8.91 (d, 1H), 7.59 (d, A [2-(benzylphenylacetylamino)- 2H), 7.51-7.41 (ca, ethoxy]phenyl}propionic acid methyl 4H), 7.33-7.09 (ca, ester 13H), 6.78-6.70 (ca, 2H), 6.65-6.55 (ca, 2H), 4.71, 4.67 (2 × s, 2H, rotamers mixture), 4.39 (q, 1H), 4.14, 3.88 (2 × t, 2H, rotamers mixture), 3.92-3.60 (ca, 7H), 3.26-3.08 (ca, 2H) IIa_172 V_2 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.26 A [3-(benzylphenylacetylamino)- MS [M + 1]⁺: 641 propoxy]phenyl}propionic acid methyl ester IIa_173 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.865 A {2-[benzyl-(2-methylacryloyl)amino]- MS [M + 1]⁺: 577 ethoxy}phenyl)propionic acid methyl ester IIa_174 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.948 A {3-[benzyl-(2-methylacryloyl)amino]- MS [M + 1]⁺: 591 propoxy}phenyl)propionic acid methyl ester IIa_175 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.367 A {2-[benzyl-(3-phenylpropynoyl)- MS [M + 1]⁺: 637 amino]ethoxy}phenyl)propionic acid methyl ester IIa_176 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.454 A {3-[benzyl-(3-phenylpropynoyl)- MS [M + 1]⁺: 651 amino]propoxy}phenyl)propionic acid methyl ester IIa_177 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.45 A {2-[benzyl-(2-ethylbutyryl)amino]- MS [M + 1]⁺: 607 ethoxy}phenyl)propionic acid methyl ester IIa_178 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.511 A {3-[benzyl-(2-ethylbutyryl)amino]- MS [M + 1]⁺: 621 propoxy}phenyl)propionic acid methyl ester IIa_179 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.087 A {2-[benzyl-(3-methylbut-2-(E)-enoyl)- MS [M + 1]⁺: 591 amino]ethoxy}phenyl)propionic acid methyl ester IIa_180 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.187 A {3-[benzyl-(3-methylbut-2-(E)-enoyl)- MS [M + 1]⁺: 605 amino]propoxy}phenyl)propionic acid methyl ester IIa_181 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.027 A {2-[benzyl-(3-furan-2-ylacryloyl)- MS [M + 1]⁺: 629 amino]ethoxy}phenyl)propionic acid methyl ester IIa_182 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.12 A {3-[benzyl-(3-furan-2-ylacryloyl)- MS [M + 1]⁺: 643 amino]propoxy}phenyl)propionic acid methyl ester IIa_183 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.19 A {2-[benzyl-(3-thiophen-2-ylacryloyl)- MS [M + 1]⁺: 645 amino]ethoxy}phenyl)propionic acid methyl ester IIa_184 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.304 A {3-[benzyl-(3-thiophen-2-ylacryloyl)- MS [M + 1]⁺: 659 amino]propoxy}phenyl)propionic acid methyl ester IIa_185 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.889 A {2-[benzyl-(3-furan-3-yl-(E)-acryloyl)- MS [M + 1]⁺: 629 amino]ethoxy}phenyl)propionic acid methyl ester IIa_186 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.005 A {3-[benzyl-(3-furan-3-yl-(E)-acryloyl)- MS [M + 1]⁺: 643 amino]propoxy}phenyl)propionic acid methyl ester IIa_187 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.097 A {2-[benzyl-(3-pyridin-3-yl-(E)- MS [M + 1]⁺: 640 acryloyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_188 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.245 A {3-[benzyl-(3-pyridin-3-yl-(E)- MS [M + 1]⁺: 654 acryloyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_189 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.105 A {2-[benzyl-(3-thiophen-3-yl-(E)- MS [M + 1]⁺: 645 acryloyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_190 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.214 A {3-[benzyl-(3-thiophen-3-yl-(E)- MS [M + 1]⁺: 659 acryloyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_191 V_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.808 A [2-(benzylbut-2-(E)-enoylamino)- MS [M + 1]⁺: 577 ethoxy]phenyl}propionic acid methyl ester IIa_192 V_2 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.336 A [3-(benzylbut-2-(E)-enoylamino)- MS [M + 1]⁺: 607 propoxy]phenyl}propionic acid methyl ester IIa_193 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.093 A {2-[benzyl-(2-thiophen-2-ylacetyl)- MS [M + 1]⁺: 633 amino]ethoxy}phenyl)propionic acid methyl ester IIa_194 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.90 (d, 1H), 7.59 (d, A {3-[benzyl-(2-thiophen-2-ylacetyl)- 2H), 7.50-7.43 (m 4H), amino]propoxy}phenyl)propionic acid 7.36-7.10 (m, 9H), methyl ester 6.91-6.74 (ca, 4H), 6.64-6.58 (ca, 2H), 4.63, 4.56 (2 × s, 2H, rotamers mixture), 4.38 (q, 1H), 3.98, 3.86 (2 × s, 2H, rotamers mixture), 3.92-3.85 (ca, 2H), 3.69 (s, 3H), 3.56, 3.47 (2 × t, 2H, rotamers mixture), 3.25-3.06 (ca, 2H), 2.06-1.90 (ca, 2H) IIa_195 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.90 (d, 1H), A {2-[benzyl-(2-pyridin-3-ylacetyl)- 8.52-8.34 (ca, 2H), 7.61-7.14 (m amino]ethoxy}phenyl)propionic acid 16H), 6.83-6.74 (ca, methyl ester 2H), 6.65-6.56 (ca, 2H), 4.74, 4.70 (2 × s, 2H, rotamers mixture), 4.40 (q, 1H), 4.15, 3.98 (2 × t, 2H, rotamers mixture), 3.93-3.66 (ca, 7H), 3.26-3.00 (ca, 2H) IIa_196 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.90 (d, 1H), A {3-[benzyl-(2-pyridin-3-ylacetyl)- 8.48-8.37 (ca, 2H), amino]propoxy}phenyl)propionic acid 7.61-7.13 (m 16H), methyl ester 6.81-6.74 (ca, 2H), 6.64-6.55 (ca, 2H), 4.63, 4.57 (2 × s, 2H, rotamers mixture), 4.38 (q, 1H), 3.92-3.88 (ca, 2H), 3.78-3.65 (ca, 5H), 3.58, 3.48 (2 × t, 2H, rotamers mixture), 3.25-3.06 (ca, 2H), 2.06-1.94 (ca, 2H) IIa_197 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.076 A {2-[benzyl-(2-thiophen-3-ylacetyl)- MS [M + 1]⁺: 633 amino]ethoxy}phenyl)propionic acid methyl ester IIa_198 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.90 (d, 1H), 7.59 (d, A {3-[benzyl-(2-thiophen-3-ylacetyl)- 2H), 7.51-7.43 (m 4H), amino]propoxy}phenyl)propionic acid 7.36-6.97 (ca, 11H), methyl ester 6.79-6.73 (ca, 2H), 6.64-6.55 (ca, 2H), 4.62, 4.52 (2 × s, 2H, rotamers mixture), 4.38 (q, 1H), 3.91-3.85 (ca, 2H), 3.80-3.69 (ca, 5H), 3.54, 3.45 (2 × t, 2H, rotamers mixture), 3.25-3.12 (ca, 2H), 2.05-1.89 (ca, 2H) IIa_199 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.502 A {2-[benzyl(3,3-dimethylbutyryl)- MS [M + 1]⁺: 607 amino]ethoxy}phenyl)propionic acid methyl ester IIa_200 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.594 A {3-[benzyl(3,3-dimethylbutyryl)- MS [M + 1]⁺: 621 amino]propoxy}phenyl)propionic acid methyl ester IIa_201 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.243 A {2-[benzyl-(3-methylbutyryl)amino]- MS [M + 1]⁺: 593 ethoxy}phenyl)propionic acid methyl ester IIa_202 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.324 A {3-[benzyl-(3-methylbutyryl)amino]- MS [M + 1]⁺: 607 propoxy}phenyl)propionic acid methyl ester IIa_203 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.90 (d, 1H), A {2-[benzyl-(3-pyridin-3-ylpropionyl)- 8.58-8.39 (ca, 2H), 7.59 (d, 2H), amino]ethoxy}phenyl)propionic acid 7.49-7.05 (ca, 14H), methyl ester 6.79-6.56 (ca, 4H), 4.68, 4.63 (2 × s, 2H, rotamers mixture), 4.39 (q, 1H), 4.11, 3.90 (2 × t, 2H, rotamers mixture), 3.75-3.57 (ca, 5H), 3.21 (dd, 1H), 3.10 (m, 1H), 3.96, 2.95 (2 × t, 2H, rotamers mixture), 2.84, 2.62 (2 × t, 2H, rotamers mixture) IIa_204 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.131 A {3-[benzyl-(3-pyridin-3-ylpropionyl)- MS [M + 1]⁺: 656 amino]propoxy}phenyl)propionic acid methyl ester IIa_205 V_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.064 A [2-(benzylpent-4-enoylamino)- MS [M + 1]⁺: 591 ethoxy]phenyl}propionic acid methyl ester IIa_206 V_2 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.159 A [3-(benzylpent-4-enoylamino)- MS [M + 1]⁺: 605 propoxy]phenyl}propionic acid methyl ester IIa_207 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.368 A {2-[benzyl-(3-phenylpropionyl)- MS [M + 1]⁺: 641 amino]ethoxy}phenyl)propionic acid methyl ester IIa_208 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.90 (d, 1H), 7.59 (d, A {3-[benzyl-(3-phenylpropionyl)- 2H), 7.50-7.04 (ca, amino]propoxy}phenyl)propionic acid 14H), 6.78-6.71 (ca, methyl ester 2H), 6.64-6.55 (ca, 2H), 4.61, 4.43 (2 × s, 2H, rotamers mixture), 4.38 (q, 1H), 3.88, 3.82 (2 × t, 2H, rotamers mixture), 3.69 (s, 3H), 3.52, 3.36 (2 × t, 2H, rotamers mixture), 3.21 (dd, 1H), 3.10 (dd, 1H), 3.02-2.90 (ca, 2H), 2.72, 2.61 (2 × t, 2H, rotamers mixture), 2.03, 1.88 (2 × t, 2H, rotamers mixture) IIa_209 V_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.19 A [2- MS [M + 1]⁺: 591 (benzylcyclobutanecarbonylamino)- ethoxy]phenyl}propionic acid methyl ester IIa_210 V_2 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.596 A [3- MS [M + 1]⁺: 621 (benzylcyclobutanecarbonylamino)- propoxy]phenyl}propionic acid methyl ester IIa_211 V_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.536 A [2- MS [M + 1]⁺: 619 (benzylcyclohexanecarbonylamino)- ethoxy]phenyl}propionic acid methyl ester IIa_212 V_2 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.624 A [3- MS [M + 1]⁺: 633 (benzylcyclohexanecarbonylamino)- propoxy]phenyl}propionic acid methyl ester IIa_213 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.056 A {2-[benzyl-(3-cyclohexylpropionyl)- MS [M + 1]⁺: 647 amino]ethoxy}phenyl)propionic acid methyl ester IIa_214 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.90 (d, 1H), 7.59 (d, A {3-[benzyl-(3-cyclohexylpropionyl)- 2H), 7.51-7.41 (ca, amino]propoxy}phenyl)propionic acid 4H), 7.31-7.13 (ca, methyl ester 8H), 6.78 (d, 2H), 6.64-6.55 (ca, 2H), 4.60, 4.52 (2 × s, 2H, rotamers mixture), 4.38 (q, 1H), 3.93-3.86 (ca, 2H), 3.69 (s, 3H), 3.52, 3.42 (2 × t, 2H, rotamers mixture), 3.25-3.08 (ca, 2H), 2.43-2.29 (ca, 2H), 2.04-1.92 (ca, 2H), 1.69-1.48 (ca, 13H) IIa_215 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.828 A {2-[benzyl-(2-cyclohexylacetyl)- MS [M + 1]⁺: 633 amino]ethoxy}phenyl)propionic acid methyl ester IIa_216 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.90 (d, 1H), 7.59 (d, A {3-[benzyl-(2-cyclohexylacetyl)- 2H), 7.51-7.41 (ca, amino]propoxy}phenyl)propionic acid 4H), 7.33-7.12 (ca, methyl ester 8H), 6.77 (d, 2H), 6.64-6.55 (ca, 2H), 4.61, 4.53 (2 × s, 2H, rotamers mixture), 4.38 (q, 1H), 3.93-3.85 (ca, 2H), 3.69 (s, 3H), 3.51, 3.44 (2 × t, 2H, rotamers mixture), 3.25-3.08 (ca, 2H), 2.26, 2.18 (2 × d, 2H, rotamers mixture), 2.04-1.92 (ca, 3H), 1.80-1.64 (ca, 10H) IIa_217 V_1 (S)-2-(2-Benzoylphenylamino)-3-{4- 8.90 (d, 1H), 7.59 (d, A [2- 2H), 7.51-7.44 (ca, (benzylcyclopentanecarbonylamino)- 4H), 7.36-7.14 (ca, ethoxy]phenyl}propionic acid methyl 8H), 6.79-6.73 (ca, ester 2H), 6.64-6.55 (ca, 2H), 4.75, 4.69 (2 × s, 2H, rotamers mixture), 4.38 (q, 1H), 4.11, 3.96 (2 × t, 2H, rotamers mixture), 3.75-3.65 (ca, 5H), 3.24-3.08 (ca, 2H), 2.75 (m, 1H), 1.87-1.74 (ca, 8H) IIa_218 V_2 (S)-2-(2-Benzoylphenylamino)-3-{4- 8.90 (d, 1H), 7.59 (d, A [3- 2H), 7.51-7.41 (ca, (benzylcyclopentanecarbonylamino)- 4H), 7.33-7.13 (ca, propoxy]phenyl}propionic acid 8H), 6.77 (d, 2H), methyl ester 6.64-6.55 (ca, 2H), 4.61, 4.59 (2 × s, 2H, rotamers mixture), 4.38 (q, 1H), 3.93-3.87 (ca, 2H), 3.69 (s, 3H), 3.53-3.44 (ca, 2H), 3.25-3.10 (ca, 2H), 2.75 (m, 1H), 1.99-1.74 (ca, 10H) IIa_219 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.814 A {2-[benzyl-(3-cyclopentylpropionyl)- MS [M + 1]⁺: 633 amino]ethoxy}phenyl)propionic acid methyl ester IIa_220 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.246 A {3-[benzyl-(3-cyclopentylpropionyl)- MS [M + 1]⁺: 605 amino]propoxy}phenyl)propionic acid methyl ester IIa_221 V_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.885 A [2- MS [M + 1]⁺: 577 (benzylcyclopropanecarbonylamino)- ethoxy]phenyl}propionic acid methyl ester IIa_222 V_2 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.969 A [3- MS [M + 1]⁺: 591 (benzylcyclopropanecarbonylamino)- propoxy]phenyl}propionic acid methyl ester IIa_223 V_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.784 A [2-(benzylpropionylamino)ethoxy]- MS [M + 1]⁺: 565 phenyl}propionic acid methyl ester IIa_224 V_2 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.858 A [3-(benzylpropionylamino)propoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid methyl ester IIa_225 V_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.02 A [2-(benzylisobutyrylamino)ethoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid methyl ester IIa_226 V_2 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.091 A [3-(benzylisobutyrylamino)propoxy]- MS [M + 1]⁺: 593 phenyl}propionic acid methyl ester IIa_227 V_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.511 A [2-(benzylhexanoylamino)ethoxy]- MS [M + 1]⁺: 607 phenyl}propionic acid methyl ester IIa_228 V_2 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.108 A [3-(benzylhexanoylamino)propoxy]- MS [M + 1]⁺: 593 phenyl}propionic acid methyl ester IIa_229 V_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.261 A [2-(benzylpentanoylamino)ethoxy]- MS [M + 1]⁺: 593 phenyl}propionic acid methyl ester IIa_230 V_2 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.337 A [3-(benzylpentanoylamino)propoxy]- MS [M + 1]⁺: 607 phenyl}propionic acid methyl ester IIa_231 V_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.027 A [2-(benzyloctanoylamino)ethoxy]- MS [M + 1]⁺: 635 phenyl}propionic acid methyl ester IIa_232 V_2 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.092 A [3-(benzyloctanoylamino)propoxy]- MS [M + 1]⁺: 649 phenyl}propionic acid methyl ester IIa_233 V_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.763 A [2-(benzylheptanoylamino)ethoxy]- MS [M + 1]⁺: 621 phenyl}propionic acid methyl ester IIa_234 V_2 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.829 A [3-(benzylheptanoylamino)propoxy]- MS [M + 1]⁺: 635 phenyl}propionic acid methyl ester IIa_235 V_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.341 A [2-(benzylnonanoylamino)ethoxy]- MS [M + 1]⁺: 649 phenyl}propionic acid methyl ester IIa_236 V_2 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.403 A [3-(benzylnonanoylamino)propoxy]- MS [M + 1]⁺: 663 phenyl}propionic acid methyl ester IIa_237 V_1 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.045 A [2-(benzylbutyrylamino)ethoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid methyl ester IIa_238 V_2 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.873 A [3-(benzylbutyrylamino)propoxy]- MS [M + 1]⁺: 647 phenyl}propionic acid methyl ester IIa_239 V_1 (S)-3-{4-[2-(Benzoylbenzylamino)- 8.90 (d, 1H), 7.59 (d, A ethoxy]phenyl}-2-(2- 2H), 7.51-7.15 (ca, benzoylphenylamino)propionic acid 17H), 6.85-6.56 (ca, methyl ester 4H), 4.87, 4.67 (2 × s, 2H, rotamers mixture), 4.39 (q, 1H), 4.24-3.56 (ca, 7H), 3.25-3.08 (ca, 2H) IIa_240 V_2 (S)-3-{4-[3-(Benzoylbenzylamino)- 8.90 (bs, 1H), 7.59 (d, A propoxy]phenyl}-2-(2- 2H), 7.51-7.14 (ca, benzoylphenylamino)propionic acid 17H), 6.83-6.55 (ca, methyl ester 4H), 4.80, 4.51 (2 × s, 2H, rotamers mixture), 4.38 (m, 1H), 4.00-3.38 (ca, 7H), 3.23 (dd, 1H), 3.11 (dd, 1H) IIa_241 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.90 (d, 1H), 7.77 (m, A {2-[benzyl-(3-phenylacryloyl)amino]- 1H), 7.59 (d, 2H), ethoxy}phenyl)propionic acid methyl 7.50-7.05 (ca, 18H), ester 6.85-6.73 (ca, 2H), 6.64-6.55 (ca, 2H), 4.86, 4.81 (2 × s, 2H, rotamers mixture), 4.38 (q, 1H), 4.20, 4.03 (2 × t, 2H, rotamers mixture), 3.85-3.68 (ca, 5H), 3.23-3.08 (ca, 2H) IIa_242 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.91 (d, 1H), 7.75 (m, A {3-[benzyl-(3-phenylacryloyl)amino]- 1H), 7.59-7.16 (ca, propoxy}phenyl)propionic acid 19H), 7.03-6.79 (ca, methyl ester 2H), 6.64-6.55 (ca, 2H), 4.73, 4.69 (2 × s, 2H, rotamers mixture), 4.38 (q, 1H), 3.98-3.91 (ca, 2H), 3.69-3.59 (ca, 5H), 3.23-3.08 (ca, 2H), 2.12-2.01 (ca, 2H) IIa_243 V_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.363 A {2-[benzyl-(2,2-dimethylpropionyl)- MS [M + 1]⁺: 593 amino]ethoxy}phenyl)propionic acid methyl ester IIa_244 V_2 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.411 A {3-[benzyl-(2,2-dimethylpropionyl)- MS [M + 1]⁺: 607 amino]propoxy}phenyl)propionic acid methyl ester IIa_245 V_3 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.408 A {2-[cyclohexyl-(3-furan-2-ylacryloyl)- MS [M + 1]⁺: 621 amino]ethoxy}phenyl)propionic acid methyl ester IIa_246 V_3 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.655 A [2- MS [M + 1]⁺: 583 (cyclobutanecarbonylcyclohexylamino) ethoxy]phenyl}propionic acid methyl ester IIa_247 V_3 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.336 A {2-[cyclohexyl-(3- MS [M + 1]⁺: 625 cyclopentylpropionyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_248 V_3 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.459 A [2-(butyrylcyclohexylamino)ethoxy]- MS [M + 1]⁺: 571 phenyl}propionic acid methyl ester IIa_249 V_5 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.272 A {2-[cyclopropylmethyl(naphthalene- MS [M + 1]⁺: 627 2-carbonyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_250 V_6 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.351 A {3-[cyclopropylmethyl(naphthalene- MS [M + 1]⁺: 641 2-carbonyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_251 V_5 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.005 A {2-[cyclopropylmethyl(quinoline-2- MS [M + 1]⁺: 628 carbonyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_252 V_6 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.065 A {3-[cyclopropylmethyl(quinoline-2- MS [M + 1]⁺: 642 carbonyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_253 V_5 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.896 A {2-[cyclopropylmethyl(quinoxaline-2- MS [M + 1]⁺: 629 carbonyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_254 V_6 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.003 A {3-[cyclopropylmethyl(quinoxaline-2- MS [M + 1]⁺: 643 carbonyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_255 V_5 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.871 A {2-[cyclopropylmethyl(thiophene-2- MS [M + 1]⁺: 583 carbonyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_256 V_6 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.976 A {3-[cyclopropylmethyl(thiophene-2- MS [M + 1]⁺: 597 carbonyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_257 V_5 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.92 A {2-[cyclopropylmethyl(pyridine-3- MS [M + 1]⁺: 578 carbonyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_258 V_6 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.062 A {3-[cyclopropylmethyl(pyridine-3- MS [M + 1]⁺: 592 carbonyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_259 V_5 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.958 A [2- MS [M + 1]⁺: 591 (cyclopropylmethylphenylacetylamino) ethoxy]phenyl}propionic acid methyl ester IIa_260 V_6 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.053 A [3- MS [M + 1]⁺: 605 (cyclopropylmethylphenylacetylamino) propoxy]phenyl}propionic acid methyl ester IIa_261 V_5 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.833 A {2-[cyclopropylmethyl-(3-furan-2- MS [M + 1]⁺: 593 ylacryloyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_262 V_6 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.934 A {3-[cyclopropylmethyl-(3-furan-2- MS [M + 1]⁺: 607 ylacryloyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_263 V_5 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.003 A {2-[cyclopropylmethyl-(3-thiophen-2- MS [M + 1]⁺: 609 ylacryloyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_264 V_6 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.11 A {3-[cyclopropylmethyl-(3-thiophen-2- MS [M + 1]⁺: 623 ylacryloyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_265 V_5 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.864 A {2-[cyclopropylmethyl-(2-thiophen-2- MS [M + 1]⁺: 597 ylacetyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_266 V_6 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.96 A {3-[cyclopropylmethyl-(2-thiophen-2- MS [M + 1]⁺: 611 ylacetyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_267 V_5 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.836 A {2-[cyclopropylmethyl-(2-thiophen-3- MS [M + 1]⁺: 597 ylacetyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_268 V_6 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.929 A {3-[cyclopropylmethyl-(2-thiophen-3- MS [M + 1]⁺: 611 ylacetyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_269 V_5 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 6.894 A {2-[cyclopropylmethyl-(3-pyridin-3- MS [M + 1]⁺: 606 ylpropionyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_270 V_6 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 6.961 A {3-[cyclopropylmethyl-(3-pyridin-3- MS [M + 1]⁺: 620 ylpropionyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_271 V_5 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.169 A {2-[cyclopropylmethyl-(3- MS [M + 1]⁺: 605 phenylpropionyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_272 V_6 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.244 A {3-[cyclopropylmethyl-(3- MS [M + 1]⁺: 619 phenylpropionyl)amino]propoxy}- phenyl)propionic acid methyl ester IIa_273 V_5 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.977 A [2- MS [M + 1]⁺: 555 (cyclobutanecarbonylcyclopropylmethylamino) ethoxy]phenyl}propionic acid methyl ester IIa_274 V_6 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.059 A [3- MS [M + 1]⁺: 569 (cyclobutanecarbonylcyclopropylmethylamino) propoxy]phenyl}propionic acid methyl ester IIa_275 V_5 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.641 A {2-[(2-cyclohexylacetyl)- MS [M + 1]⁺: 597 cyclopropylmethylamino]ethoxy}- phenyl)propionic acid methyl ester IIa_276 V_6 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.707 A {3-[(2-cyclohexylacetyl)- MS [M + 1]⁺: 611 cyclopropylmethylamino]propoxy}- phenyl)propionic acid methyl ester IIa_277 V_5 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.201 A [2- MS [M + 1]⁺: 569 (cyclopentanecarbonylcyclopropylmethylamino) ethoxy]phenyl}propionic acid methyl ester IIa_278 V_6 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.285 A [3- MS [M + 1]⁺: 583 (cyclopentanecarbonylcyclopropylmethylamino) propoxy]phenyl}propionic acid methyl ester IIa_279 V_5 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.641 A [2- MS [M + 1]⁺: 541 (cyclopropanecarbonylcyclopropylmethylamino) ethoxy]phenyl}propionic acid methyl ester IIa_280 V_6 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.747 A [3- MS [M + 1]⁺: 555 (cyclopropanecarbonylcyclopropylmethylamino) propoxy]phenyl}propionic acid methyl ester IIa_281 V_5 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.525 A [2- MS [M + 1]⁺: 529 (cyclopropylmethylpropionylamino)- ethoxy]phenyl}propionic acid methyl ester IIa_282 V_6 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.626 A [3- MS [M + 1]⁺: 543 (cyclopropylmethylpropionylamino)- propoxy]phenyl}propionic acid methyl ester IIa_283 V_5 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.791 A [2- MS [M + 1]⁺: 543 (cyclopropylmethylisobutyrylamino)- ethoxy]phenyl}propionic acid methyl ester IIa_284 V_6 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.895 A [3- MS [M + 1]⁺: 557 (cyclopropylmethylisobutyrylamino)- propoxy]phenyl}propionic acid methyl ester IIa_285 V_5 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.813 A [2-(butyrylcyclopropylmethylamino)- MS [M + 1]⁺: 543 ethoxy]phenyl}propionic acid methyl ester IIa_286 V_6 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.903 A [3-(butyrylcyclopropylmethylamino)- MS [M + 1]⁺: 557 propoxy]phenyl}propionic acid methyl ester IIa_287 V_5 (S)-3-{4-[2- rt: 8.858 A (Benzoylcyclopropylmethylamino)- MS [M + 1]⁺: 577 ethoxy]phenyl}-2-(2- benzoylphenylamino)propionic acid methyl ester IIa_288 V_6 (S)-3-{4-[3- rt: 8.958 A (Benzoylcyclopropylmethylamino)- MS [M + 1]⁺: 591 propoxy]phenyl}-2-(2- benzoylphenylamino)propionic acid methyl ester IIa_289 V_5 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.085 A {2-[cyclopropylmethyl-(3- MS [M + 1]⁺: 602 phenylacryloyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_290 V_6 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.182 A {3-[cyclopropylmethyl-(3- MS [M + 1]⁺: 617 phenylacryloyl)amino]propoxy}- phenyl)propionic acid methyl ester IIa_291 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.13 A {2-[(naphthalene-1-carbonyl)- MS [M + 1]⁺: 649 phenylamino]ethoxy}phenyl)- propionic acid methyl ester IIa_292 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.283 A {3-[(naphthalene-1-carbonyl)- MS [M + 1]⁺: 663 phenylamino]propoxy}phenyl)- propionic acid methyl ester IIa_293 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.315 A {2-[(naphthalene-2-carbonyl)- MS [M + 1]⁺: 649 phenylamino]ethoxy}phenyl)- propionic acid methyl ester IIa_294 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.429 A {3-[(naphthalene-2-carbonyl)- MS [M + 1]⁺: 663 phenylamino]propoxy}phenyl)- propionic acid methyl ester IIa_295 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.904 A {2-[phenyl(quinoline-2-carbonyl)- MS [M + 1]⁺: 650 amino]ethoxy}phenyl)propionic acid methyl ester IIa_296 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.023 A {3-[phenyl(quinoline-2-carbonyl)- MS [M + 1]⁺: 664 amino]propoxy}phenyl)propionic acid methyl ester IIa_297 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.817 A {2-[phenyl(quinoxaline-2-carbonyl)- MS [M + 1]⁺: 651 amino]ethoxy}phenyl)propionic acid methyl ester IIa_298 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.976 A {3-[phenyl(quinoxaline-2-carbonyl)- MS [M + 1]⁺: 665 amino]propoxy}phenyl)propionic acid methyl ester IIa_299 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.049 A {2-[phenyl(thiophene-2-carbonyl)- MS [M + 1]⁺: 605 amino]ethoxy}phenyl)propionic acid methyl ester IIa_300 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.155 A {3-[phenyl(thiophene-2-carbonyl)- MS [M + 1]⁺: 619 amino]propoxy}phenyl)propionic acid methyl ester IIa_301 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.746 A {2-[(isoquinoline-3-carbonyl)- MS [M + 1]⁺: 650 phenylamino]ethoxy}phenyl)- propionic acid methyl ester IIa_302 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.086 A {2-[phenyl(pyridine-3-carbonyl)- MS [M + 1]⁺: 600 amino]ethoxy}phenyl)propionic acid methyl ester IIa_303 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.264 A {3-[phenyl(pyridine-3-carbonyl)- MS [M + 1]⁺: 614 amino]propoxy}phenyl)propionic acid methyl ester IIa_304 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.934 A {2-[phenyl(pyridine-4-carbonyl)- MS [M + 1]⁺: 600 amino]ethoxy}phenyl)propionic acid methyl ester IIa_305 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.124 A {3-[phenyl(pyridine-4-carbonyl)- MS [M + 1]⁺: 614 amino]propoxy}phenyl)propionic acid methyl ester IIa_306 V_9 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.22 A [2-(phenylphenylacetylamino)- MS [M + 1]⁺: 613 ethoxy]phenyl}propionic acid methyl ester IIa_307 V_10 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.363 A [3-(phenylphenylacetylamino)- MS [M + 1]⁺: 627 propoxy]phenyl}propionic acid methyl ester IIa_308 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.799 A {2-[(2-methylacryloyl)phenylamino]- MS [M + 1]⁺: 563 ethoxy}phenyl)propionic acid methyl ester IIa_309 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.943 A {3-[(2-methylacryloyl)phenylamino]- MS [M + 1]⁺: 577 propoxy}phenyl)propionic acid methyl ester IIa_310 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.245 A {2-[phenyl-(3-phenylpropynoyl)- MS [M + 1]⁺: 615 amino]ethoxy}phenyl)propionic acid methyl ester IIa_311 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.5 A {2-[(2-ethylbutyryl)phenylamino]- MS [M + 1]⁺: 593 ethoxy}phenyl)propionic acid methyl ester IIa_312 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.628 A {3-[(2-ethylbutyryl)phenylamino]- MS [M + 1]⁺: 607 propoxy}phenyl)propionic acid methyl ester IIa_313 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.025 A {2-[(3-furan-2-ylacryloyl)- MS [M + 1]⁺: 615 phenylamino]ethoxy}phenyl)- propionic acid methyl ester IIa_314 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.164 A {3-[(3-furan-2-ylacryloyl)- MS [M + 1]⁺: 629 phenylamino]propoxy}phenyl)- propionic acid methyl ester IIa_315 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.267 A {2-[phenyl-(3-thiophen-2-ylacryloyl)- MS [M + 1]⁺: 631 amino]ethoxy}phenyl)propionic acid methyl ester IIa_316 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.394 A {3-[phenyl-(3-thiophen-2-ylacryloyl)- MS [M + 1]⁺: 645 amino]propoxy}phenyl)propionic acid methyl ester IIa_317 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.954 A {2-[(3-furan-3-yl-(E)-acryloyl)- MS [M + 1]⁺: 615 phenylamino]ethoxy}phenyl)- propionic acid methyl ester IIa_318 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.091 A {3-[(3-furan-3-yl-(E)-acryloyl)- MS [M + 1]⁺: 629 phenylamino]propoxy}-phenyl)- propionic acid methyl ester IIa_319 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.103 A {2-[phenyl-(3-pyridin-3-yl-(E)- MS [M + 1]⁺: 626 acryloyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_320 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.293 A {3-[phenyl-(3-pyridin-3-yl-(E)- MS [M + 1]⁺: 640 acryloyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_321 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.213 A {2-[phenyl-(3-thiophen-3-yl-(E)- MS [M + 1]⁺: 631 acryloyl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_322 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.334 A {3-[phenyl-(3-thiophen-3-yl-(E)- MS [M + 1]⁺: 645 acryloyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_323 V_10 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9 A [3-(but-2-(E)-enoylphenylamino)- MS [M + 1]⁺: 577 propoxy]phenyl}propionic acid methyl ester IIa_324 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.132 A {2-[phenyl-(2-thiophen-2-ylacetyl)- MS [M + 1]⁺: 619 amino]ethoxy}phenyl)propionic acid methyl ester IIa_325 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.295 A {3-[phenyl-(2-thiophen-2-ylacetyl)- MS [M + 1]⁺: 633 amino]propoxy}phenyl)propionic acid methyl ester IIa_326 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.23 A {3-[phenyl-(2-thiophen-3-ylacetyl)- MS [M + 1]⁺: 633 amino]propoxy}phenyl)propionic acid methyl ester IIa_327 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.587 A {2-[(3,3-dimethylbutyryl)- MS [M + 1]⁺: 593 phenylamino]ethoxy}phenyl)- propionic acid methyl ester IIa_328 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.706 A {3-[(3,3-dimethylbutyryl)- MS [M + 1]⁺: 607 phenylamino]propoxy}phenyl)- propionic acid methyl ester IIa_329 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.271 A {2-[(3-methylbutyryl)phenylamino]- MS [M + 1]⁺: 579 ethoxy}phenyl)propionic acid methyl ester IIa_330 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.401 A {3-[(3-methylbutyryl)phenylamino]- MS [M + 1]⁺: 593 propoxy}phenyl)propionic acid methyl ester IIa_331 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.038 A {2-[phenyl-(3-pyridin-3-ylpropionyl)- MS [M + 1]⁺: 627 amino]ethoxy}phenyl)propionic acid methyl ester IIa_332 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.229 A {3-[phenyl-(3-pyridin-3-ylpropionyl)- MS [M + 1]⁺: 641 amino]propoxy}phenyl)propionic acid methyl ester IIa_333 V_9 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.078 A [2-(pent-4-enoylphenylamino)- MS [M + 1]⁺: 577 ethoxy]phenyl}propionic acid methyl ester IIa_334 V_10 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.212 A [3-(pent-4-enoylphenylamino)- MS [M + 1]⁺: 591 propoxy]phenyl}propionic acid methyl ester IIa_335 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.369 A {2-[phenyl-(3-phenylpropionyl)- MS [M + 1]⁺: 627 amino]ethoxy}phenyl)propionic acid methyl ester IIa_336 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.494 A {3-[phenyl-(3-phenylpropionyl)- MS [M + 1]⁺: 641 amino]propoxy}phenyl)propionic acid methyl ester IIa_337 V_9 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.203 A [2- MS [M + 1]⁺: 577 (cyclobutanecarbonylphenylamino)- ethoxy]phenyl}propionic acid methyl ester IIa_338 V_10 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.333 A [3- MS [M + 1]⁺: 591 (cyclobutanecarbonylphenylamino)- propoxy]phenyl}propionic acid methyl ester IIa_339 V_9 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.602 A [2- MS [M + 1]⁺: 605 (cyclohexanecarbonylphenylamino)- ethoxy]phenyl}propionic acid methyl ester IIa_340 V_10 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.708 A [3- MS [M + 1]⁺: 619 (cyclohexanecarbonylphenylamino)- propoxy]phenyl}propionic acid methyl ester IIa_341 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.166 A {2-[(3-cyclohexylpropionyl)- MS [M + 1]⁺: 633 phenylamino]ethoxy}phenyl)- propionic acid methyl ester IIa_342 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.282 A {3-[(3-cyclohexylpropionyl)- MS [M + 1]⁺: 647 phenylamino]propoxy}phenyl)- propionic acid methyl ester IIa_343 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.883 A {2-[(2-cyclohexylacetyl)- MS [M + 1]⁺: 619 phenylamino]ethoxy}phenyl)- propionic acid methyl ester IIa_344 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10 A {3-[(2-cyclohexylacetyl)- MS [M + 1]⁺: 633 phenylamino]propoxy}phenyl)- propionic acid methyl ester IIa_345 V_9 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.463 A [2- MS [M + 1]⁺: 591 (cyclopentanecarbonylphenylamino)- ethoxy]phenyl}propionic acid methyl ester IIa_346 V_10 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.582 A [3- MS [M + 1]⁺: 605 (cyclopentanecarbonylphenylamino)- propoxy]phenyl}propionic acid methyl ester IIa_347 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.87 A {2-[(3-cyclopentylpropionyl)- MS [M + 1]⁺: 619 phenylamino]ethoxy}phenyl)- propionic acid methyl ester IIa_348 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.98 A {3-[(3-cyclopentylpropionyl)- MS [M + 1]⁺: 633 phenylamino]propoxy}phenyl)- propionic acid methyl ester IIa_349 V_9 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.91 A [2- MS [M + 1]⁺: 563 (cyclopropanecarbonylphenylamino)- ethoxy]phenyl}propionic acid methyl ester IIa_350 V_10 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.06 A [3- MS [M + 1]⁺: 577 (cyclopropanecarbonylphenylamino)- propoxy]phenyl}propionic acid methyl ester IIa_351 V_9 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.78 A [2-(phenylpropionylamino)ethoxy]- MS [M + 1]⁺: 551 phenyl}propionic acid methyl ester IIa_352 V_10 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.925 A [3-(phenylpropionylamino)propoxy]- MS [M + 1]⁺: 565 phenyl}propionic acid methyl ester IIa_353 V_9 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.033 A [2-(isobutyrylphenylamino)ethoxy]- MS [M + 1]⁺: 565 phenyl}propionic acid methyl ester IIa_354 V_10 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.168 A [3-(isobutyrylphenylamino)propoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid methyl ester IIa_355 V_9 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.56 A [2-(hexanoylphenylamino)ethoxy]- MS [M + 1]⁺: 593 phenyl}propionic acid methyl ester IIa_356 V_10 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.671 A [3-(hexanoylphenylamino)propoxy]- MS [M + 1]⁺: 607 phenyl}propionic acid methyl ester IIa_357 V_9 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.298 A [2-(pentanoylphenylamino)ethoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid methyl ester IIa_358 V_10 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.421 A [3-(pentanoylphenylamino)propoxy]- MS [M + 1]⁺: 593 phenyl}propionic acid methyl ester IIa_359 V_9 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.11 A [2-(octanoylphenylamino)ethoxy]- MS [M + 1]⁺: 621 phenyl}propionic acid methyl ester IIa_360 V_10 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.224 A [3-(octanoylphenylamino)propoxy]- MS [M + 1]⁺: 635 phenyl}propionic acid methyl ester IIa_361 V_9 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.825 A [2-(heptanoylphenylamino)ethoxy]- MS [M + 1]⁺: 607 phenyl}propionic acid methyl ester IIa_362 V_10 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.933 A [3-(heptanoylphenylamino)propoxy]- MS [M + 1]⁺: 621 phenyl}propionic acid methyl ester IIa_363 V_9 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.455 A [2-(nonanoylphenylamino)ethoxy]- MS [M + 1]⁺: 635 phenyl}propionic acid methyl ester IIa_364 V_10 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 10.588 A [3-(nonanoylphenylamino)propoxy]- MS [M + 1]⁺: 649 phenyl}propionic acid methyl ester IIa_365 V_9 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.043 A [2-(butyrylphenylamino)ethoxy]- MS [M + 1]⁺: 565 phenyl}propionic acid methyl ester IIa_366 V_10 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.18 A [3-(butyrylphenylamino)propoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid methyl ester IIa_367 V_9 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.97 A [2-(benzoylphenylamino)ethoxy]- MS [M + 1]⁺: 599 phenyl}propionic acid methyl ester IIa_368 V_10 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.121 A [3-(benzoylphenylamino)propoxy]- MS [M + 1]⁺: 613 phenyl}propionic acid methyl ester IIa_369 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.383 A {2-[phenyl-(3-phenylacryloyl)amino]- MS [M + 1]⁺: 625 ethoxy}phenyl)propionic acid methyl ester IIa_370 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.51 A {3-[phenyl-(3-phenylacryloyl)amino]- MS [M + 1]⁺: 639 propoxy}phenyl)propionic acid methyl ester IIa_371 V_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.402 A {2-[(2,2-dimethylpropionyl)- MS [M + 1]⁺: 579 phenylamino]ethoxy}phenyl)- propionic acid methyl ester IIa_372 V_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.5 A {3-[(2,2-dimethylpropionyl)- MS [M + 1]⁺: 593 phenylamino]propoxy}phenyl)- propionic acid methyl ester IIa_373 V_4 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.256 A [2-(tert- MS [M + 1]⁺: 557 butylcyclobutanecarbonylamino)- ethoxy]phenyl}propionic acid methyl ester IIa_374 V_4 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.917 A {2-[tert-butyl-(3- MS [M + 1]⁺: 599 cyclopentylpropionyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_375 V_26 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.214 A {2-[(2-methylacryloyl)naphthalen-1- MS [M + 1]⁺: 613 ylamino]ethoxy}phenyl)propionic acid methyl ester IIa_376 V_26 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.276 A [2-(but-2-(E)-enoylnaphthalen-1- MS [M + 1]⁺: 613 ylamino)ethoxy]phenyl}propionic acid methyl ester IIa_377 V_26 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.336 A [2- MS [M + 1]⁺: 613 (cyclopropanecarbonylnaphthalen-1- ylamino)ethoxy]phenyl}propionic acid methyl ester IIa_378 V_26 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.273 A [2-(naphthalen-1-ylpropionylamino)- MS [M + 1]⁺: 601 ethoxy]phenyl}propionic acid methyl ester IIa_379 V_30 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.261 A {2-[(2-methylacryloyl)naphthalen-2- MS [M + 1]⁺: 613 ylamino]ethoxy}phenyl)propionic acid methyl ester IIa_380 V_30 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.355 A [2-(but-2-(E)-enoylnaphthalen-2- MS [M + 1]⁺: 613 ylamino)ethoxy]phenyl}propionic acid methyl ester IIa_381 V_30 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.269 A [2-(naphthalen-2-ylpropionylamino)- MS [M + 1]⁺: 601 ethoxy]phenyl}propionic acid methyl ester IIa_382 V_30 (S)-3-{4-[2-(Acetylnaphthalen-2- rt: 8.914 A ylamino)ethoxy]phenyl}-2-(2- MS [M + 1]⁺: 587 benzoylphenylamino)propionic acid methyl ester IIa_383 V_27 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.054 A {2-[(2-methylacryloyl)-(3- MS [M + 1]⁺: 609 methylsulfanylphenyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_384 V_27 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.126 A {2-[but-2-(E)-enoyl-(3- MS [M + 1]⁺: 609 methylsulfanylphenyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_385 V_27 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.28 A {2-[butyryl-(3-methylsulfanylphenyl)- MS [M + 1]⁺: 611 amino]ethoxy}phenyl)propionic acid methyl ester IIa_386 V_28 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.051 A {2-[(2-methylacryloyl)-(4- MS [M + 1]⁺: 609 methylsulfanylphenyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_387 V_28 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.134 A {2-[but-2-(E)-enoyl-(4- MS [M + 1]⁺: 609 methylsulfanylphenyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_388 V_28 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.284 A {2-[isobutyryl-(4- MS [M + 1]⁺: 611 methylsulfanylphenyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_389 V_28 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.284 A {2-[butyryl-(4-methylsulfanylphenyl)- MS [M + 1]⁺: 611 amino]ethoxy}phenyl)propionic acid methyl ester IIa_390 V_26 (S)-3-{4-[2-(Acetylnaphthalen-1- rt: 8.903 A ylamino)ethoxy]phenyl}-2-(2- MS [M + 1]⁺: 587 benzoylphenylamino)propionic acid methyl ester IIa_391 V_30 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.387 A [2- MS [M + 1]⁺: 613 (cyclopropanecarbonylnaphthalen-2- ylamino)ethoxy]phenyl}propionic acid methyl ester IIa_392 V_31 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.23 A {3-[butyryl-(2-fluorophenyl)amino]- MS [M + 1]⁺: 597 propoxy}phenyl)propionic acid methyl ester IIa_393 V_31 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.355 A {3-[cyclobutanecarbonyl-(2- MS [M + 1]⁺: 609 fluorophenyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_394 V_31 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.056 A {3-[cyclopropanecarbonyl-(2- MS [M + 1]⁺: 595 fluorophenyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_395 V_31 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.219 A {3-[(2-fluorophenyl)isobutyrylamino]- MS [M + 1]⁺: 597 propoxy}phenyl)propionic acid methyl ester IIa_396 V_1 (S)-3-{4-[2-(Acryloylbenzylamino)- rt: 8.639 A ethoxy]phenyl}-2-(2- MS [M + 1]⁺: 563 benzoylphenylamino)propionic acid methyl ester IIa_397 V_2 (S)-3-{4-[3-(Acryloylbenzylamino)- rt: 8.747 A propoxy]phenyl}-2-(2- MS [M + 1]⁺: 577 benzoylphenylamino)propionic acid methyl ester IIa_398 V_9 (S)-3-{4-[2-(Acryloylphenylamino)- rt: 8.693 A ethoxy]phenyl}-2-(2- MS [M + 1]⁺: 549 benzoylphenylamino)propionic acid methyl ester IIa_399 V_10 (S)-3-{4-[2-(Acryloylphenylamino)- rt: 8.842 A propoxy]phenyl}-2-(2- MS [M + 1]⁺: 563 benzoylphenylamino)propionic acid methyl ester IIa_400 V_31 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.986 A {3-[(2-fluorophenyl)propionylamino]- MS [M + 1]⁺: 583 propoxy}phenyl)propionic acid methyl ester IIa_401 V_31 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.279 A {3-[(2-fluorophenyl)pent-4- MS [M + 1]⁺: 609 enoylamino]propoxy}phenyl)- propionic acid methyl ester IIa_402 V_31 (S)-3-(4-{3-[Acryloyl-(2- rt: 8.87 A fluorophenyl)amino]propoxy}phenyl)- MS [M + 1]⁺: 581 2-(2-benzoylphenylamino)propionic acid methyl ester IIa_403 V_31 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.009 A {3-[but-2-(E)-enoyl-(2-fluorophenyl)- MS [M + 1]⁺: 595 amino]propoxy}phenyl)propionic acid methyl ester IIa_404 V_31 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.45 A {3-[(2-fluorophenyl)-(3- MS [M + 1]⁺: 611 methylbutyryl)amino]propoxy}- phenyl)propionic acid methyl ester IIa_405 V_29 (R)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.023 A {2-[phenyl(thiophene-2-carbonyl)- MS [M + 1]⁺: 605 amino]ethoxy}phenyl)propionic acid methyl ester IIa_406 V_31 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.048 A {3-[(2-fluorophenyl)-(2- MS [M + 1]⁺: 595 methylacryloyl)amino]propoxy}- phenyl)propionic acid methyl ester IIa_407 V_32 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.025 A {3-[(3-fluorophenyl)-(2- MS [M + 1]⁺: 595 methylacryloyl)amino]propoxy}- phenyl)propionic acid methyl ester IIa_408 V_34 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.84 A {2-[but-2-(E)-enoyl-(2- MS [M + 1]⁺: 593 methoxyphenyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_409 V_35 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.852 A {2-[but-2-(E)-enoyl-(3- MS [M + 1]⁺: 593 methoxyphenyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_410 V_34 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.303 A {2-[(2-methoxyphenyl)-(3- MS [M + 1]⁺: 609 methylbutyryl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_411 V_32 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.436 A {3-[(3-fluorophenyl)-(3- MS [M + 1]⁺: 611 methylbutyryl)amino]propoxy}- phenyl)propionic acid methyl ester IIa_412 V_35 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.243 A {2-[(3-methoxyphenyl)-(3- MS [M + 1]⁺: 609 methylbutyryl)amino]ethoxy}phenyl)- propionic acid methyl ester IIa_413 V_32 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.262 A {3-[(3-fluorophenyl)pent-4- MS [M + 1]⁺: 609 enoylamino]propoxy}phenyl)- propionic acid methyl ester IIa_414 V_32 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.353 A {3-[cyclobutanecarbonyl-(3- MS [M + 1]⁺: 609 fluorophenyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_415 V_33 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.338 A {3-[cyclobutanecarbonyl-(4- MS [M + 1]⁺: 609 fluorophenyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_416 V_29 (R)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.207 A [2- MS [M + 1]⁺: 577 (cyclobutanecarbonylphenylamino)- ethoxy]phenyl}propionic acid methyl ester IIa_417 V_34 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.891 A {2-[cyclopropanecarbonyl-(2- MS [M + 1]⁺: 593 methoxyphenyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_418 V_32 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.103 A {3-[cyclopropanecarbonyl-(3- MS [M + 1]⁺: 595 fluorophenyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_419 V_33 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.082 A {3-[cyclopropanecarbonyl-(4- MS [M + 1]⁺: 595 fluorophenyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_420 V_34 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.817 A {2-[(2-methoxyphenyl)- MS [M + 1]⁺: 581 propionylamino]ethoxy}phenyl)- propionic acid methyl ester IIa_421 V_32 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.976 A {3-[(3-fluorophenyl)propionylamino]- MS [M + 1]⁺: 583 propoxy}phenyl)propionic acid methyl ester IIa_422 V_35 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.766 A {2-[(3-methoxyphenyl)- MS [M + 1]⁺: 581 propionylamino]ethoxy}phenyl)- propionic acid methyl ester IIa_423 V_33 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.958 A {3-[(4-fluorophenyl)propionylamino]- MS [M + 1]⁺: 583 propoxy}phenyl)propionic acid methyl ester IIa_424 V_29 (R)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.783 A [2-(phenylpropionylamino)ethoxy]- MS [M + 1]⁺: 551 phenyl}propionic acid methyl ester IIa_425 V_32 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.206 A {3-[(3-fluorophenyl)isobutyrylamino]- MS [M + 1]⁺: 597 propoxy}phenyl)propionic acid methyl ester IIa_426 V_35 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.011 A {2-[isobutyryl-(3-methoxyphenyl)- MS [M + 1]⁺: 595 amino]ethoxy}phenyl)propionic acid methyl ester IIa_427 V_33 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.187 A {3-[(4-fluorophenyl)isobutyrylamino]- MS [M + 1]⁺: 597 propoxy}phenyl)propionic acid methyl ester IIa_428 V_31 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.473 A {3-[(2-fluorophenyl)pentanoylamino]- MS [M + 1]⁺: 611 propoxy}phenyl)propionic acid methyl ester IIa_429 V_32 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.455 A {3-[(3-fluorophenyl)pentanoylamino]- MS [M + 1]⁺: 611 propoxy}phenyl)propionic acid methyl ester IIa_430 V_34 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.069 A {2-[butyryl-(2-methoxyphenyl)amino]- MS [M + 1]⁺: 595 ethoxy}phenyl)propionic acid methyl ester IIa_431 V_32 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.227 A {3-[butyryl-(3-fluorophenyl)amino]- MS [M + 1]⁺: 597 propoxy}phenyl)propionic acid methyl ester IIa_432 V_35 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.014 A {2-[butyryl-(3-methoxyphenyl)amino]- MS [M + 1]⁺: 595 ethoxy}phenyl)propionic acid methyl ester IIa_433 V_33 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.202 A {3-[butyryl-(4-fluorophenyl)amino]- MS [M + 1]⁺: 597 propoxy}phenyl)propionic acid methyl ester IIa_434 V_31 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.539 A {3-[(2,2-dimethylpropionyl)-(2- MS [M + 1]⁺: 611 fluorophenyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_435 V_34 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.411 A {2-[(2,2-dimethylpropionyl)-(2- MS [M + 1]⁺: 609 methoxyphenyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_436 V_32 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.518 A {3-[(2,2-dimethylpropionyl)-(3- MS [M + 1]⁺: 611 fluorophenyl)amino]propoxy}phenyl)- propionic acid methyl ester IIa_437 V_35 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.367 A {2-[(2,2-dimethylpropionyl)-(3- MS [M + 1]⁺: 609 methoxyphenyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_438 V_27 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.277 A {2-[isobutyryl-(3- MS [M + 1]⁺: 611 methylsulfanylphenyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_439 V_37 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.92 A {3-[(2-methoxyphenyl)- MS [M + 1]⁺: 595 propionylamino]propoxy}phenyl)- propionic acid methyl ester IIa_440 V_37 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.154 A {3-[cyclopropanecarbonyl-(2- MS [M + 1]⁺: 609 methoxyphenyl)amino]propoxy}- phenyl)propionic acid methyl ester IIa_441 V_37 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.999 A {3-[isobutyryl-(2-methoxyphenyl)- MS [M + 1]⁺: 607 amino]propoxy}phenyl)propionic acid methyl ester IIa_442 V_37 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.942 A {3-[but-2-(E)-enoyl-(2- MS [M + 1]⁺: 607 methoxyphenyl)amino]propoxy}- phenyl)propionic acid methyl ester IIa_443 V_37 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.954 A {3-[(2-methoxyphenyl)-(2- MS [M + 1]⁺: 607 methylacryloyl)amino]propoxy}- phenyl)propionic acid methyl ester IIa_444 V_37 (S)-3-(4-{3-[Acryloyl-(2- rt: 8.82 A methoxyphenyl)amino]propoxy}- MS [M + 1]⁺: 593 phenyl)-2-(2-benzoylphenylamino)- propionic acid methyl ester IIa_445 V_37 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.161 A {3-[butyryl-(2-methoxyphenyl)amino]- MS [M + 1]⁺: 609 propoxy}phenyl)propionic acid methyl ester IIa_446 V_38 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.904 A {3-[(3-methoxyphenyl)- MS [M + 1]⁺: 595 propionylamino]propoxy}phenyl)- propionic acid methyl ester IIa_447 V_38 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.029 A {3-[cyclopropanecarbonyl-(3- MS [M + 1]⁺: 607 methoxyphenyl)amino]propoxy}- phenyl)propionic acid methyl ester IIa_448 V_38 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.137 A {3-[isobutyryl-(3-methoxyphenyl)- MS [M + 1]⁺: 609 amino]propoxy}phenyl)propionic acid methyl ester IIa_449 V_38 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.98 A {3-[but-2-(E)-enoyl-(3- MS [M + 1]⁺: 607 methoxyphenyl)amino]propoxy}- phenyl)propionic acid methyl ester IIa_450 V_38 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.923 A {3-[(3-methoxyphenyl)-(2- MS [M + 1]⁺: 607 methylacryloyl)amino]propoxy}- phenyl)propionic acid methyl ester IIa_451 V_38 (S)-3-(4-{3-[Acryloyl-(3- rt: 8.845 A methoxyphenyl)amino]propoxy}- MS [M + 1]⁺: 593 phenyl)-2-(2-benzoylphenylamino)- propionic acid methyl ester IIa_452 V_38 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.143 A {3-[butyryl-(3-methoxyphenyl)amino]- MS [M + 1]⁺: 609 propoxy}phenyl)propionic acid methyl ester IIa_453 V_34 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.202 A {2-[cyclobutanecarbonyl-(2- MS [M + 1]⁺: 607 methoxyphenyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_454 V_34 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.066 A {2-[isobutyryl-(2-methoxyphenyl)- MS [M + 1]⁺: 595 amino]ethoxy}phenyl)propionic acid methyl ester IIa_455 V_26 (S)-3-{4-[2-(Acryloylnaphthalen-1- rt: 9.145 A ylamino)ethoxy]phenyl}-2-(2- MS [M + 1]⁺: 599 benzoylphenylamino)propionic acid methyl ester IIa_456 V_30 (S)-3-{4-[2-(Acryloylnaphthalen-2- rt: 9.201 A ylamino)ethoxy]phenyl}-2-(2- MS [M + 1]⁺: 599 benzoylphenylamino)propionic acid methyl ester IIa_457 V_27 (S)-3-(4-{2-[Acryloyl-(3- rt: 8.979 A methylsulfanylphenyl)amino]ethoxy}- MS [M + 1]⁺: 595 phenyl)-2-(2-benzoylphenylamino)- propionic acid methyl ester IIa_458 V_28 (S)-3-(4-{2-[Acryloyl-(4- rt: 8.982 A methylsulfanylphenyl)amino]ethoxy}- MS [M + 1]⁺: 595 phenyl)-2-(2-benzoylphenylamino)- propionic acid methyl ester IIa_459 V_32 (S)-3-(4-{3-[Acryloyl-(3- rt: 8.908 A fluorophenyl)amino]propoxy}phenyl)- MS [M + 1]⁺: 581 2-(2-benzoylphenylamino)propionic acid methyl ester IIa_460 V_32 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.06 A {3-[but-2-(E)-enoyl-(3-fluorophenyl)- MS [M + 1]⁺: 595 amino]propoxy}phenyl)propionic acid methyl ester IIa_461 V_34 (S)-3-(4-{2-[Acryloyl-(2- rt: 8.709 A methoxyphenyl)amino]ethoxy}- MS [M + 1]⁺: 579 phenyl)-2-(2-benzoylphenylamino)- propionic acid methyl ester IIa_462 V_34 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.85 A {2-[(2-methoxyphenyl)-(2- MS [M + 1]⁺: 593 methylacryloyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_463 V_35 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.887 A {2-[cyclopropanecarbonyl-(3- MS [M + 1]⁺: 593 methoxyphenyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_464 V_35 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.164 A {2-[cyclobutanecarbonyl-(3- MS [M + 1]⁺: 607 methoxyphenyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_465 V_35 (S)-3-(4-{2-[Acryloyl-(3- rt: 8.703 A methoxyphenyl)amino]ethoxy}- MS [M + 1]⁺: 579 phenyl)-2-(2-benzoylphenylamino)- propionic acid methyl ester IIa_466 V_35 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.786 A {2-[(3-methoxyphenyl)-(2- MS [M + 1]⁺: 593 methylacryloyl)amino]ethoxy}- phenyl)propionic acid methyl ester IIa_467 V_36 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.001 A {2-[ethyl(naphthalene-2-carbonyl)- MS [M + 1]⁺: 601 amino]ethoxy}phenyl)propionic acid methyl ester IIa_468 V_39 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.244 A {2-[(naphthalene-2-carbonyl)- MS [M + 1]⁺: 615 propylamino]ethoxy}phenyl)propionic acid methyl ester IIa_469 V_36 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.712 A {2-[ethyl(quinoline-2-carbonyl)- MS [M + 1]⁺: 602 amino]ethoxy}phenyl)propionic acid methyl ester IIa_470 V_39 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.999 A {2-[propyl(quinoline-2-carbonyl)- MS [M + 1]⁺: 616 amino]ethoxy}phenyl)propionic acid methyl ester IIa_471 V_36 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.595 A {2-[ethyl(quinoxaline-2-carbonyl)- MS [M + 1]⁺: 603 amino]ethoxy}phenyl)propionic acid methyl ester IIa_472 V_39 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.888 A {2-[propyl(quinoxaline-2-carbonyl)- MS [M + 1]⁺: 617 amino]ethoxy}phenyl)propionic acid methyl ester IIa_473 V_36 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.558 A {2-[ethyl(thiophene-2-carbonyl)- MS [M + 1]⁺: 557 amino]ethoxy}phenyl)propionic acid methyl ester IIa_474 V_39 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.841 A {2-[propyl(thiophene-2-carbonyl)- MS [M + 1]⁺: 571 amino]ethoxy}phenyl)propionic acid methyl ester IIa_475 V_36 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.545 A {2-[ethyl(pyridine-3-carbonyl)amino]- MS [M + 1]⁺: 552 ethoxy}phenyl)propionic acid methyl ester IIa_476 V_39 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.863 A {2-[propyl(pyridine-3-carbonyl)- MS [M + 1]⁺: 566 amino]ethoxy}phenyl)propionic acid methyl ester IIa_477 V_36 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.711 A {2-[ethyl-(3-thiophen-2-ylacryloyl)- MS [M + 1]⁺: 583 amino]ethoxy}phenyl)propionic acid methyl ester IIa_478 V_39 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.993 A {2-[propyl-(3-thiophen-2-ylacryloyl)- MS [M + 1]⁺: 597 amino]ethoxy}phenyl)propionic acid methyl ester IIa_479 V_39 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.34 A {2-[(3,3-dimethylbutyryl)- MS [M + 1]⁺: 559 propylamino]ethoxy}phenyl)propionic acid methyl ester IIa_480 V_36 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 6.512 A {2-[ethyl-(3-pyridin-3-ylpropionyl)- MS [M + 1]⁺: 580 amino]ethoxy}phenyl)propionic acid methyl ester IIa_481 V_39 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 6.767 A {2-[propyl-(3-pyridin-3-ylpropionyl)- MS [M + 1]⁺: 594 amino]ethoxy}phenyl)propionic acid methyl ester IIa_482 V_39 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.955 A [2- MS [M + 1]⁺: 543 (cyclobutanecarbonylpropylamino)- ethoxy]phenyl}propionic acid methyl ester IIa_483 V_39 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.789 A [2-(isobutyrylpropylamino)ethoxy]- MS [M + 1]⁺: 531 phenyl}propionic acid methyl ester IIa_484 V_39 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.775 A [2-(butyrylpropylamino)ethoxy]- MS [M + 1]⁺: 531 phenyl}propionic acid methyl ester IIa_485 V_36 (S)-3-{4-[2-(Benzoylethylamino)- rt: 8.547 A ethoxy]phenyl}-2-(2- MS [M + 1]⁺: 551 benzoylphenylamino)propionic acid methyl ester IIa_486 V_39 (S)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.829 A [2-(benzoylpropylamino)ethoxy]- MS [M + 1]⁺: 565 phenyl}propionic acid methyl ester IIa_487 V_36 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.806 A {2-[ethyl-(3-phenylacryloyl)amino]- MS [M + 1]⁺: 577 ethoxy}phenyl)propionic acid methyl ester IIa_488 V_36 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.931 A {2-[(2,2-dimethylpropionyl)- MS [M + 1]⁺: 531 ethylamino]ethoxy}phenyl)propionic acid methyl ester IIa_489 V_39 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.233 A {2-[(2,2-dimethylpropionyl)- MS [M + 1]⁺: 545 propylamino]ethoxy}phenyl)propionic acid methyl ester IIa_490 V_24 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.298 A {3-[(3-chlorophenyl)-(2- MS [M, M + 2]⁺: 611, methylacryloyl)amino]propoxy}- 613 phenyl)propionic acid methyl ester IIa_491 V_25 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.347 A {3-[(3-chlorophenyl)-(2- MS [M, M + 2]⁺: 611, methylacryloyl)amino]propoxy}- 613 phenyl)propionic acid methyl ester

Compounds I:

Compounds I described shown in Table 6 were obtained starting from the corresponding ester derivative of formula II following any of the procedures J or K described below.

PROCEDURE J: To a 0.02 M solution of compound II (1 eq) in a mixture of THF:methanol (3:1) or THF, a 1 M aqueous solution of lithium hydroxide (1.5 eq) was added. The resulting mixture was stirred at room temperature for 18 h, then treated with HCl 1 N until pH=5-6, and extracted twice with EtOAc. The organic layers were dried over anhydrous sodium sulfate and filtered. The solvent was distilled off under reduced pressure.

PROCEDURE K: To a solution 0.03 M of compound II (1 eq) in methanol, potassium hydroxide (10 eq) was added. The resulting solution was stirred at room temperature for 18 h, then treated with HCl 1 N until acid pH=4-5. To the resulting suspension, water and EtOAc were added. The organic layer was separated and the aqueous layer was extracted once with EtOAc. The combined organic layers were dried over anhydrous sodium sulfate and filtered. The solvent was distilled off under reduced pressure.

TABLE 6 Example Starting HPLC Number product Compound name ¹H-NMR/LC-MS Method I_1 IIa_1 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.327 A {2-[(2-chlorophenyl)-(2- MS [M, M + 2]⁺: 583, 585 methylacryloyl)amino]ethoxy}phenyl)- propionic acid I_2 IIa_2 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.476 A {3-[(2-chlorophenyl)-(2- MS [M, M + 2]⁺: 597, 599 methylacryloyl)amino]propoxy}- phenyl)propionic acid I_3 IIa_3 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.295 A {2-[but-2-(E)-enoyl-(2-chlorophenyl)- MS [M, M + 2]⁺: 583, 585 amino]ethoxy}phenyl)propionic acid I_4 IIa_4 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.855 A {2-[(2-chlorophenyl)-(3-methylbutyryl)- MS [M, M + 2]⁺: 599, 601 amino]ethoxy}phenyl)propionic acid I_5 IIa_5 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.728 A {2-[(2-chlorophenyl)- MS [M, M + 2]⁺: 597, 599 cyclobutanecarbonylamino]ethoxy}- phenyl)propionic acid I_6 IIa_6 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.989 A {2-[(2-chlorophenyl)- MS [M, M + 2]⁺: 611, 613 cyclopentanecarbonylamino]ethoxy}- phenyl)propionic acid I_7 IIa_7 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.353; MS [M, M + 2]⁺: A {2-[(2-chlorophenyl)- 583, 585 cyclopropanecarbonylamino]ethoxy}- phenyl)propionic acid I_8 IIa_8 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.508 A {3-[(2-chlorophenyl)- MS [M, M + 2]⁺: 597, 599 cyclopropanecarbonylamino]propoxy}- phenyl)propionic acid I_9 IIa_9 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.298 A {2-[(2-chlorophenyl)propionylamino]- MS [M, M + 2]⁺: 571, 573 ethoxy}phenyl)propionic acid I_10 IIa_10 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.446 A {3-[(2-chlorophenyl)propionylamino]- MS [M, M + 2]⁺: 585, 587 propoxy}phenyl)propionic acid I_11 IIa_11 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.561 A {2-[(2-chlorophenyl)isobutyrylamino]- MS [M, M + 2]⁺: 585, 587 ethoxy}phenyl)propionic acid I_12 IIa_12 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.701 A {3-[(2-chlorophenyl)isobutyrylamino]- MS [M, M + 2]⁺: 599, 601 propoxy}phenyl)propionic acid I_13 IIa_13 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.588 A {2-[butyryl-(2-chlorophenyl)amino]- MS [M, M + 2]⁺: 585, 587 ethoxy}phenyl)propionic acid I_14 IIa_14 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.726 A {3-[butyryl-(2-chlorophenyl)amino]- MS [M, M + 2]⁺: 599, 601 propoxy}phenyl)propionic acid I_15 IIa_15 (S)-3-(4-{3-[Acryloyl-(2-chlorophenyl)- rt: 8.293 A amino]propoxy}phenyl)-2-(2- MS [M, M + 2]⁺: 583, 585 benzoylphenylamino)propionic acid I_16 IIa_16 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.19 A {2-[(2-fluorophenyl)-(thiophene-2- MS [M + 1]⁺: 609 carbonyl)amino]ethoxy}phenyl)- propionic acid I_17 IIa_17 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.054 A {2-[(2-fluorophenyl)-(2- MS [M + 1]⁺: 567 methylacryloyl)amino]ethoxy}phenyl)- propionic acid I_18 IIa_18 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.534 A {2-[(2-fluorophenyl)-(3-methylbutyryl)- MS [M + 1]⁺: 583 amino]ethoxy}phenyl)propionic acid I_19 IIa_19 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.414 A {2-[cyclobutanecarbonyl-(2- MS [M + 1]⁺: 581 fluorophenyl)amino]ethoxy}phenyl)- propionic acid I_20 IIa_20 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.674 A {2-[cyclopentanecarbonyl-(2- MS [M + 1]⁺: 595 fluorophenyl)amino]ethoxyl}phenyl)- propionic acid I_21 IIa_21 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.061 A {2-[cyclopropanecarbonyl-(2- MS [M + 1]⁺: 567 fluorophenyl)amino]ethoxy}phenyl)- propionic acid I_22 IIa_22 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.981 A {2-[(2-fluorophenyl)propionylamino]- MS [M + 1]⁺: 555 ethoxy}phenyl)propionic acid I_23 IIa_23 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.256 A {2-[(2-fluorophenyl)isobutyrylamino]- MS [M + 1]⁺: 569 ethoxy}phenyl)propionic acid I_24 IIa_24 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.269 A {2-[butyryl-(2-fluorophenyl)amino]- MS [M + 1]⁺: 569 ethoxy}phenyl)propionic acid I_25 IIa_25 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.665 A {2-[(2,2-dimethylpropionyl)-(2- MS [M + 1]⁺: 583 fluorophenyl)amino]ethoxy}phenyl)- propionic acid I_26 IIa_26 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.369 A {3-[(2-methylacryloyl)-o-tolylamino]- MS [M + 1]⁺: 577 propoxy}phenyl)propionic acid I_27 IIa_27 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.99 A {2-[(2-ethylbutyryl)-o-tolylamino]- MS [M + 1]⁺: 593 ethoxy}phenyl)propionic acid I_28 IIa_28 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.758 A {3-[(3-methylbut-2-(E)-enoyl)-o- MS [M + 1]⁺: 591 tolylamino]propoxy}phenyl)propionic acid I_29 IIa_29 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.471 A (but-2-(E)-enoyl-o-tolylamino)- MS [M + 1]⁺: 577 propoxy]phenyl}propionic acid I_30 IIa_30 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.101 A {2-[(3,3-dimethylbutyryl)-o-tolylamino]- MS [M + 1]⁺: 593 ethoxy}phenyl)propionic acid I_31 IIa_31 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.75 A {2-[(3-methylbutyryl)-o-tolylamino]- MS [M + 1]⁺: 579 ethoxy}phenyl)propionic acid I_32 IIa_32 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.945 A {3-[(3-methylbutyryl)-o-tolylamino]- MS [M + 1]⁺: 593 propoxy}phenyl)propionic acid I_33 IIa_33 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.742 A (o-tolylpent-4-enoylamino)propoxy]- MS [M + 1]⁺: 591 phenyl}propionic acid I_34 IIa_34 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.634 A (cyclobutanecarbonyl-o-tolylamino)- MS [M + 1]⁺: 577 ethoxy]phenyl}propionic acid I_35 IIa_35 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.898 A (cyclopentanecarbonyl-o-tolylamino)- MS [M + 1]⁺: 591 ethoxy]phenyl}propionic acid I_36 IIa_36 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.387 A (propionyl-o-tolylamino)propoxy]- MS [M + 1]⁺: 565 phenyl}propionic acid I_37 IIa_37 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.458 A (isobutyryl-o-tolylamino)ethoxy]- MS [M + 1]⁺: 565 phenyl}propionic acid I_38 IIa_38 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.66 A (isobutyryl-o-tolylamino)propoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid I_39 IIa_39 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.968 A (pentanoyl-o-tolylamino)propoxy]- MS [M + 1]⁺: 593 phenyl}propionic acid I_40 IIa_40 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.474 A (butyryl-o-tolylamino)ethoxy]phenyl}- MS [M + 1]⁺: 565 propionic acid I_41 IIa_41 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.677 A (butyryl-o-tolylamino)propoxy]phenyl}- MS [M + 1]⁺: 579 propionic acid I_42 IIa_42 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.324 A (benzoyl-o-tolylamino)ethoxy]phenyl}- MS [M + 1]⁺: 599 propionic acid I_43 IIa_43 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.884 A {2-[(2,2-dimethylpropionyl)-o- MS [M + 1]⁺: 579 tolylamino]ethoxy}phenyl)propionic acid I_44 IIa_44 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.028 A {3-[(2,2-dimethylpropionyl)-o- MS [M + 1]⁺: 593 tolylamino]propoxy}phenyl)propionic acid I_45 IIa_45 (S)-3-{4-[3-(Acryloyl-o-tolylamino)- rt: 8.31 A propoxy]phenyl}-2-(2- MS [M + 1]⁺: 563 benzoylphenylamino)propionic acid I_46 IIa_46 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.385 A {2-[(3-chlorophenyl)-(2- MS [M, M + 2]⁺: 583, 586 methylacryloyl)amino]ethoxy}phenyl)- propionic acid I_47 IIa_490 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.54 A {3-[(3-chlorophenyl)-(2- MS [M, M + 2]⁺: 597, 599 methylacryloyl)amino]propoxy}- phenyl)propionic acid I_48 IIa_47 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.45 A {2-[but-2-(E)-enoyl-(3-chlorophenyl)- MS [M, M + 2]⁺: 583, 585 amino]ethoxy}phenyl)propionic acid I_49 IIa_48 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.596 A {3-[but-2-(E)-enoyl-(3-chlorophenyl)- MS [M, M + 2]⁺: 597, 599 amino]propoxy}phenyl)propionic acid I_50 IIa_49 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.877 A {2-[(3-chlorophenyl)-(3-methylbutyryl)- MS [M, M + 2]⁺: 599, 601 amino]ethoxy}phenyl)propionic acid I_51 IIa_50 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.68 A {2-[(3-chlorophenyl)-pent-4- MS [M, M + 2]⁺: 597, 599 enoylamino]ethoxy}phenyl)propionic acid I_52 IIa_51 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.787 A {2-[(3-chlorophenyl)- MS [M, M + 2]⁺: 597, 599 cyclobutanecarbonylamino]ethoxy}- phenyl)propionic acid I_53 IIa_52 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.040 A {2-[(3-chlorophenyl)- MS [M, M + 2]⁺: 611, 613 cyclopentanecarbonylamino]ethoxy}- phenyl)propionic acid I_54 IIa_53 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.481 A {2-[(3-chlorophenyl)- MS [M, M + 2]⁺: 583, 585 cyclopropanecarbonylamino]ethoxy}- phenyl)propionic acid I_55 IIa_54 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.645; MS [M, M + 2]⁺: A {3-[(3-chlorophenyl)- 597, 599 cyclopropanecarbonylamino]propoxy}- phenyl)propionic acid I_56 IIa_55 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.345 A {2-[(3-chlorophenyl)propioylamino]- MS [M, M + 2]⁺: 571, 573 ethoxy}phenyl)propionic acid I_57 IIa_56 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.509 A {3-[(3-chlorophenyl)propionylamino]- MS [M, M + 2]⁺: 585, 587 propoxy}phenyl)propionic acid I_58 IIa_57 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.613 A {2-[(3-chlorophenyl)isobutyrylamino]- MS [M, M + 2]⁺: 585, 587 ethoxy}phenyl)propionic acid I_59 IIa_58 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.768 A {3-[(3-chlorophenyl)isobutyrylamino]- MS [M, M + 2]⁺: 599, 601 propoxy}phenyl)propionic acid I_60 IIa_59 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.623 A {2-[butyryl-(3-chlorophenyl)amino]- MS [M, M + 2]⁺: 585, 587 ethoxy}phenyl)propionic acid I_61 IIa_60 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.779; MS [M, M + 2]⁺: A {3-[butyryl-(3-chlorophenyl)amino]- 599, 601 propoxy}phenyl)propionic acid I_62 IIa_61 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.995 A {2-[(3-chlorophenyl)-(2,2- MS [M, M + 2]⁺: 599, 601 dimethylpropionyl)amino]ethoxy}- phenyl)propionic acid I_63 IIa_62 (S)-3-(4-{3-[Acryloyl-(3-chlorophenyl)- rt: 8.419 A amino]propoxy}phenyl)-2-(2- MS [M, M + 2]⁺: 583, 585 benzoylphenylamino)propionic acid I_64 IIa_63 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.250 A {2-[(3-fluorophenyl)-(thiophene-2- MS [M + 1]⁺: 609 carbonyl)amino]ethoxy}phenyl)- propionic acid I_65 IIa_64 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.062 A {2-[(3-fluorophenyl)-(2- MS [M + 1]⁺: 567 methylacryloyl)amino]ethoxy}phenyl)- propionic acid I_66 IIa_65 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.538 A {2-[(3-fluorophenyl)-(3-methylbutyryl)- MS [M + 1]⁺: 583 amino]ethoxy}phenyl)propionic acid I_67 IIa_66 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.431 A {2-[cyclobutanecarbonyl-(3- MS [M + 1]⁺: 581 fluorophenyl)amino]ethoxy}phenyl)- propionic acid I_68 IIa_67 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.688 A {2-[cyclopentanecarbonyl-(3- MS [M + 1]⁺: 595 fluorophenyl)amino]ethoxy}phenyl)- propionic acid I_69 IIa_68 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.134 A {2-[cyclopropanecarbonyl-(3- MS [M + 1]⁺: 567 fluorophenyl)amino]ethoxy}phenyl)- propionic acid I_70 IIa_69 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.998 A {2-[(3-fluorophenyl)propionylamino]- MS [M + 1]⁺: 555 ethoxy}phenyl)propionic acid I_71 IIa_70 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.267 A {2-[(3-fluorophenyl)isobutyrylamino]- MS [M + 1]⁺: 569 ethoxy}phenyl)propionic acid I_72 IIa_71 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.278 A {2-[butyryl-(3-fluorophenyl)amino]- MS [M + 1]⁺: 569 ethoxy}phenyl)propionic acid I_73 IIa_72 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.65 A {2-[(2,2-dimethylpropionyl)-(3- MS [M + 1]⁺: 583 fluorophenyl)amino]ethoxy}phenyl)- propionic acid I_74 IIa_73 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.439 A {3-[(2-methylacryloyl)-(3- MS [M + 1]⁺: 591 methylbenzyl)amino]propoxy}phenyl)- propionic acid I_75 IIa_74 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.973 A {2-[(2-ethylbutyryl)-(3-methylbenzyl)- MS [M + 1]⁺: 607 amino]ethoxy}phenyl)propionic acid I_76 IIa_75 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.634 A {3-[(3-methylbenzyl)-(3-methylbut-2- MS [M + 1]⁺: 605 (E)-enoyl)amino]propoxy}phenyl)- propionic acid I_77 IIa_76 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.381 A {3-[but-2-(E)-enoyl-(3-methylbenzyl)- MS [M + 1]⁺: 591 amino]propoxy}phenyl)propionic acid I_78 IIa_77 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.041 A {2-[(3,3-dimethylbutyryl)-(3- MS [M + 1]⁺: 607 methylbenzyl)amino]ethoxy}phenyl)- propionic acid I_79 IIa_78 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.745 A {2-[(3-methylbenzyl)-(3- MS [M + 1]⁺: 593 methylbutyryl)amino]ethoxy}phenyl)- propionic acid I_80 IIa_79 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.828 A {3-[(3-methylbenzyl)-(3- MS [M + 1]⁺: 607 methylbutyryl)amino]propoxy}phenyl)- propionic acid I_81 IIa_80 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.645 A {2-[cyclobutanecarbonyl-(3- MS [M + 1]⁺: 591 methylbenzyl)amino]ethoxy}phenyl)- propionic acid I_82 IIa_81 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.722 A {3-[cyclobutanecarbonyl-(3- MS [M + 1]⁺: 605 methylbenzyl)amino]propoxy}phenyl)- propionic acid I_83 IIa_82 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.874 A {2-[cyclopentanecarbonyl-(3- MS [M + 1]⁺: 605 methylbenzyl)amino]ethoxy}phenyl)- propionic acid I_84 IIa_83 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.422 A {3-[cyclopropanecarbonyl-(3- MS [M + 1]⁺: 591 methylbenzyl)amino]propoxy}phenyl)- propionic acid I_85 IIa_84 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.31 A {3-[(3-methylbenzyl)propionylamino]- MS [M + 1]⁺: 579 propoxy}phenyl)propionic acid I_86 IIa_85 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.468 A {2-[isobutyryl-(3-methylbenzyl)amino]- MS [M + 1]⁺: 579 ethoxy}phenyl)propionic acid I_87 IIa_86 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.56 A {3-[isobutyryl-(3-methylbenzyl)amino]- MS [M + 1]⁺: 593 propoxy}phenyl)propionic acid I_88 IIa_87 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.489 A {2-[butyryl-(3-methylbenzyl)amino]- MS [M + 1]⁺: 579 ethoxy}phenyl)propionic acid I_89 IIa_88 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.574 A {3-[butyryl-(3-methylbenzyl)amino]- MS [M + 1]⁺: 593 propoxy}phenyl)propionic acid I_90 IIa_89 (S)-3-(4-{2-[Benzoyl-(3-methylbenzyl)- rt: 8.545 A amino]ethoxy}phenyl)-2-(2- MS [M + 1]⁺: 613 benzoylphenylamino)propionic acid I_91 IIa_90 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.886 A {2-[(2,2-dimethylpropionyl)-(3- MS [M + 1]⁺: 593 methylbenzyl)amino]ethoxy}phenyl)- propionic acid I_92 IIa_91 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.909 A {3-[(2,2-dimethylpropionyl)-(3- MS [M + 1]⁺: 607 methylbenzyl)amino]propoxy}phenyl)- propionic acid I_93 IIa_92 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.472 A {3-[(2-methylacryloyl)-m-tolylamino]- MS [M + 1]⁺: 577 propoxy}phenyl)propionic acid I_94 IIa_93 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.062 A {2-[(2-ethylbutyryl)-m-tolylamino]- MS [M + 1]⁺: 593 ethoxy}phenyl)propionic acid I_95 IIa_94 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.826 A {3-[(3-methylbut-2-(E)-enoyl)-m- MS [M + 1]⁺: 591 tolylamino]propoxy}phenyl)propionic acid I_96 IIa_95 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.554 A (but-2-(E)-enoyl-m-tolylamino)- MS [M + 1]⁺: 577 propoxy]phenyl}propionic acid I_97 IIa_96 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.152 A {2-[(3,3-dimethylbutyryl)-m- MS [M + 1]⁺: 593 tolylamino]ethoxy}phenyl)propionic acid I_98 IIa_97 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.802 A {2-[(3-methylbutyryl)-m-tolylamino]- MS [M + 1]⁺: 579 ethoxy}phenyl)propionic acid I_99 IIa_98 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.724 A (cyclobutanecarbonyl-m-tolylamino)- MS [M + 1]⁺: 577 ethoxy]phenyl}propionic acid I_100 IIa_99 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.958 A (cyclopentanecarbonyl-m-tolylamino)- MS [M + 1]⁺: 591 ethoxy]phenyl}propionic acid I_101 IIa_100 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.607 A (cyclopropanecarbonyl-m-tolylamino)- MS [M + 1]⁺: 577 propoxy]phenyl}propionic acid I_102 IIa_101 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.468 A (propionyl-m-tolylamino)propoxy]- MS [M + 1]⁺: 565 phenyl}propionic acid I_103 IIa_102 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.532 A (isobutyryl-m-tolylamino)ethoxy]- MS [M + 1]⁺: 565 phenyl}propionic acid I_104 IIa_103 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.731 A (isobutyryl-m-tolylamino)propoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid I_105 IIa_104 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 9.025 A (pentanoyl-m-tolylamino)propoxy]- MS [M + 1]⁺: 593 phenyl}propionic acid I_106 IIa_105 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.543 A (butyryl-m-tolylamino)ethoxy]phenyl}- MS [M + 1]⁺: 565 propionic acid I_107 IIa_106 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.741 A (butyryl-m-tolylamino)propoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid I_108 IIa_107 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.436 A (benzoyl-m-tolylamino)ethoxy]phenyl}- MS [M + 1]⁺: 599 propionic acid I_109 IIa_108 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.953 A {2-[(2,2-dimethylpropionyl)-m- MS [M + 1]⁺: 579 tolylamino]ethoxy}phenyl)propionic acid I_110 IIa_109 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.109 A {3-[(2,2-dimethylpropionyl)-m- MS [M + 1]⁺: 593 tolylamino]propoxy}phenyl)propionic acid I_111 IIa_110 (S)-3-{4-[3-(Acryloyl-m-tolylamino)- rt: 8.388 A propoxy]phenyl}-2-(2- MS [M + 1]⁺: 563 benzoylphenylamino)propionic acid I_112 IIa_111 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.437 A {2-[(4-chlorophenyl)-(2- MS [M, M + 2]⁺: 583, 586 methylacryloyl)amino]ethoxy}phenyl)- propionic acid I_113 IIa_491 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.595 A {3-[(4-chlorophenyl)-(2- MS [M, M + 2]⁺: 597, 599 methylacryloyl)amino]propoxy}- phenyl)propionic acid I_114 IIa_112 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.517 A {2-[but-2-(E)-enoyl-(4-chlorophenyl)- MS [M, M + 2]⁺: 583, 585 amino]ethoxy}phenyl)propionic acid I_115 IIa_113 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.942 A {2-[(4-chlorophenyl)-(3-methylbutyryl)- MS [M, M + 2]⁺: 599, 601 amino]ethoxy}phenyl)propionic acid I_116 IIa_114 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.739 A {2-[(4-chlorophenyl)-pent-4- MS [M, M + 2]⁺: 597, 599 enoylamino]ethoxy}phenyl)propionic acid I_117 IIa_115 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.839 A {2-[(4-chlorophenyl)- MS [M, M + 2]⁺: 597, 599 cyclobutanecarbonylamino]ethoxy}- phenyl)propionic acid I_118 IIa_116 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.103 A {2-[(4-chlorophenyl)- MS [M, M + 2]⁺: 611, 613 cyclopentanecarbonylamino]ethoxy}- phenyl)propionic acid I_119 IIa_117 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.533 A {2-[(4-chlorophenyl)- MS [M, M + 2]⁺: 583, 585 cyclopropanecarbonylamino]ethoxy}- phenyl)propionic acid I_120 IIa_118 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.696 A {3-[(4-chlorophenyl)- MS [M, M + 2]⁺: 597, 599 cyclopropanecarbonylamino]propoxy}- phenyl)propionic acid I_121 IIa_119 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.399 A {2-[(4-chlorophenyl)propionylamino]- MS [M, M + 2]⁺: 571, 573 ethoxy}phenyl)propionic acid I_122 IIa_120 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.562 A {3-[(4-chlorophenyl)propionylamino]- MS [M, M + 2]⁺: 585, 587 propoxy}phenyl)propionic acid I_123 IIa_121 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.682 A {2-[(4-chlorophenyl)isobutyrylamino]- MS [M, M + 2]⁺: 585, 587 ethoxy}phenyl)propionic acid I_124 IIa_122 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.835 A {3-[(4-chlorophenyl)isobutyrylamino]- MS [M, M + 2]⁺: 599, 601 propoxy}phenyl)propionic acid I_125 IIa_123 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.684 A {2-[butyryl-(4-chlorophenyl)amino]- MS [M, M + 2]⁺: 585, 587 ethoxy}phenyl)propionic acid I_126 IIa_124 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.836 A {3-[butyryl-(4-chlorophenyl)amino]- MS [M, M + 2]⁺: 599, 601 propoxy}phenyl)propionic acid I_127 IIa_125 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.043 A {2-[(4-chlorophenyl)-(2,2- MS [M, M + 2]⁺: 599, 601 dimethylpropionyl)amino]ethoxy}- phenyl)propionic acid I_128 IIa_126 (S)-3-(4-{3-[Acryloyl-(4-chlorophenyl)- rt: 8.475 A amino]propoxy}phenyl)-2-(2- MS [M, M + 2]⁺: 583, 585 benzoylphenylamino)propionic acid I_129 IIa_127 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.247 A {2-[(4-fluorophenyl)-(thiophene-2- MS [M + 1]⁺: 609 carbonyl)amino]ethoxy}phenyl)- propionic acid I_130 IIa_128 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.026 A {2-[(4-fluorophenyl)-(2- MS [M + 1]⁺: 567 methylacryloyl)amino]ethoxy}phenyl)- propionic acid I_131 IIa_129 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.365 A {2-[(4-fluorophenyl)-(3-methylbut-2- MS [M + 1]⁺: 581 (E)-enoyl)amino]ethoxy}phenyl)- propionic acid I_132 IIa_130 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.528 A {2-[(4-fluorophenyl)-(3-methylbutyryl)- MS [M + 1]⁺: 583 amino]ethoxy}phenyl)propionic acid I_133 IIa_131 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.421 A {2-[cyclobutanecarbonyl-(4- MS [M + 1]⁺: 581 fluorophenyl)amino]ethoxy}phenyl)- propionic acid I_134 IIa_132 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.675 A {2-[cyclopentanecarbonyl-(4- MS [M + 1]⁺: 595 fluorophenyl)amino]ethoxy}phenyl)- propionic acid I_135 IIa_133 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.117 A {2-[cyclopropanecarbonyl-(4- MS [M + 1]⁺: 567 fluorophenyl)amino]ethoxy}phenyl)- propionic acid I_136 IIa_134 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.987 A {2-[(4-fluorophenyl)propionylamino]- MS [M + 1]⁺: 555 ethoxy}phenyl)propionic acid I_137 IIa_135 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.253 A {2-[(4-fluorophenyl)isobutyrylamino]- MS [M + 1]⁺: 569 ethoxy}phenyl)propionic acid I_138 IIa_136 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.266 A {2-[butyryl-(4-fluorophenyl)amino]- MS [M + 1]⁺: 569 ethoxy}phenyl)propionic acid I_139 IIa_137 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.64 A {2-[(2,2-dimethylpropionyl)-(4- MS [M + 1]⁺: 583 fluorophenyl)amino]ethoxy}phenyl)- propionic acid I_140 IIa_138 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.483 A {3-[(2-methylacryloyl)-p-tolylamino]- MS [M + 1]⁺: 577 propoxy}phenyl)propionic acid I_141 IIa_139 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.088 A {2-[(2-ethylbutyryl)-p-tolylamino]- MS [M + 1]⁺: 593 ethoxy}phenyl)propionic acid I_142 IIa_140 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.178 A {2-[(3,3-dimethylbutyryl)-p-tolylamino]- MS [M + 1]⁺: 593 ethoxy}phenyl)propionic acid I_143 IIa_141 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.827 A {2-[(3-methylbutyryl)-p-tolylamino]- MS [M + 1]⁺: 579 ethoxy}phenyl)propionic acid I_144 IIa_142 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.025 A {3-[(3-methylbutyryl)-p-tolylamino]- MS [M + 1]⁺: 593 propoxy}phenyl)propionic acid I_145 IIa_143 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.737 A (cyclobutanecarbonyl-p-tolylamino)- MS [M + 1]⁺: 577 ethoxy]phenyl}propionic acid I_146 IIa_144 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.936 A (cyclobutanecarbonyl-p-tolylamino)- MS [M + 1]⁺: 591 propoxy]phenyl}propionic acid I_147 IIa_145 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.992 A (cyclopentanecarbonyl-p-tolylamino)- MS [M + 1]⁺: 591 ethoxy]phenyl}propionic acid I_148 IIa_146 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.486 A (propionyl-p-tolylamino)propoxy]- MS [M + 1]⁺: 565 phenyl}propionic acid I_149 IIa_147 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.554 A (isobutyryl-p-tolylamino)ethoxy]- MS [M + 1]⁺: 565 phenyl}propionic acid I_150 IIa_148 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.758 A (isobutyryl-p-tolylamino)propoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid I_151 IIa_149 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.561 A (butyryl-p-tolylamino)ethoxy]phenyl}- MS [M + 1]⁺: 565 propionic acid I_152 IIa_150 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.431 A (benzoyl-p-tolylamino)ethoxy]phenyl}- MS [M + 1]⁺: 599 propionic acid I_153 IIa_151 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.967 A {2-[(2,2-dimethylpropionyl)-p- MS [M + 1]⁺: 579 tolylamino]ethoxy}phenyl)propionic acid I_154 IIa_152 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.126 A {3-[(2,2-dimethylpropionyl)-p- MS [M + 1]⁺: 593 tolylamino]propoxy}phenyl)propionic acid I_155 IIa_153 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.702 A {2-[benzyl(naphthalene-1-carbonyl)- MS [M + 1]⁺: 649 amino]ethoxy}phenyl)propionic acid I_156 IIa_154 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.744 A {2-[benzyl(naphthalene-2-carbonyl)- MS [M + 1]⁺: 649 amino]ethoxy}phenyl)propionic acid I_157 IIa_155 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.713 A {2-[benzyl(pyrazine-2-carbonyl)- MS [M + 1]⁺: 601 amino]ethoxy}phenyl)propionic acid I_158 IIa_156 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.813 A {3-[benzyl(pyrazine-2-carbonyl)- MS [M + 1]⁺: 615 amino]propoxy}phenyl)propionic acid I_159 IIa_157 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.866 A {2-[benzyl(pyridine-2-carbonyl)amino]- MS [M + 1]⁺: 600 ethoxy}phenyl)propionic acid I_160 IIa_158 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.978 A {3-[benzyl(pyridine-2-carbonyl)amino]- MS [M + 1]⁺: 614 propoxy}phenyl)propionic acid I_161 IIa_159 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.538 A {2-[benzyl(quinoline-2-carbonyl)- MS [M + 1]⁺: 650 amino]ethoxy}phenyl)propionic acid I_162 IIa_160 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.602 A {3-[benzyl(quinoline-2-carbonyl)- MS [M + 1]⁺: 664 amino]propoxy}phenyl)propionic acid I_163 IIa_161 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.374 A {2-[benzyl(quinoxaline-2-carbonyl)- MS [M + 1]⁺: 651 amino]ethoxy}phenyl)propionic acid I_164 IIa_162 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.455 A {3-[benzyl(quinoxaline-2-carbonyl)- MS [M + 1]⁺: 665 amino]propoxy}phenyl)propionic acid I_165 IIa_163 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.331 A {2-[benzyl(thiophene-2-carbonyl)- MS [M + 1]⁺: 605 amino]ethoxy}phenyl)propionic acid I_166 IIa_164 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.415 A {3-[benzyl(thiophene-2-carbonyl)- MS [M + 1]⁺: 619 amino]propoxy}phenyl)propionic acid I_167 IIa_165 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.026 A {2-[benzyl(furan-3-carbonyl)amino]- MS [M + 1]⁺: 589 ethoxy}phenyl)propionic acid I_168 IIa_166 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.105 A {3-[benzyl(furan-3-carbonyl)amino]- MS [M + 1]⁺: 603 propoxy}phenyl)propionic acid I_169 IIa_167 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.318 A {2-[benzyl(isoquinoline-3-carbonyl)- MS [M + 1]⁺: 650 amino]ethoxy}phenyl)propionic acid I_170 IIa_168 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.383 A {3-[benzyl(isoquinoline-3-carbonyl)- MS [M + 1]⁺: 664 amino]propoxy}phenyl)propionic acid I_171 IIa_169 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.448 A {2-[benzyl(pyridine-3-carbonyl)amino]- MS [M + 1]⁺: 600 ethoxy}phenyl)propionic acid I_172 IIa_170 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.584 A {3-[benzyl(pyridine-3-carbonyl)amino]- MS [M + 1]⁺: 614 propoxy}phenyl)propionic acid I_173 IIa_171 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.461 A (benzylphenylacetylamino)ethoxy]- MS [M + 1]⁺: 613 phenyl}propionic acid I_174 IIa_172 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.489 A (benzylphenylacetylamino)propoxy]- MS [M + 1]⁺: 627 phenyl}propionic acid I_175 IIa_173 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.057 A {2-[benzyl-(2-methylacryloyl)amino]- MS [M + 1]⁺: 563 ethoxy}phenyl)propionic acid I_176 IIa_174 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.14 A {3-[benzyl-(2-methylacryloyl)amino]- MS [M + 1]⁺: 577 propoxy}phenyl)propionic acid I_177 IIa_175 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.675 A {2-[benzyl-(3-phenylpropynoyl)amino]- MS [M + 1]⁺: 623 ethoxy}phenyl)propionic acid I_178 IIa_176 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.762 A {3-[benzyl-(3-phenylpropynoyl)amino]- MS [M + 1]⁺: 637 propoxy}phenyl)propionic acid I_179 IIa_177 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.711 A {2-[benzyl-(2-ethylbutyryl)amino]- MS [M + 1]⁺: 593 ethoxy}phenyl)propionic acid I_180 IIa_178 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.766 A {3-[benzyl-(2-ethylbutyryl)amino]- MS [M + 1]⁺: 607 propoxy}phenyl)propionic acid I_181 IIa_179 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.278 A {2-[benzyl-(3-methylbut-2-(E)-enoyl)- MS [M + 1]⁺: 577 amino]ethoxy}phenyl)propionic acid I_182 IIa_180 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.381 A {3-[benzyl-(3-methylbut-2-(E)-enoyl)- MS [M + 1]⁺: 591 amino]propoxy}phenyl)propionic acid I_183 IIa_181 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.279 A {2-[benzyl-(3-furan-2-ylacryloyl)- MS [M + 1]⁺: 615 amino]ethoxy}phenyl)propionic acid I_184 IIa_182 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.386 A {3-[benzyl-(3-furan-2-ylacryloyl)- MS [M + 1]⁺: 629 amino]propoxy}phenyl)propionic acid I_185 IIa_183 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.436 A {2-[benzyl-(3-thiophen-2-ylacryloyl)- MS [M + 1]⁺: 631 amino]ethoxy}phenyl)propionic acid I_186 IIa_184 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.551 A {3-[benzyl-(3-thiophen-2-ylacryloyl)- MS [M + 1]⁺: 645 amino]propoxy}phenyl)propionic acid I_187 IIa_185 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.158 A {2-[benzyl-(3-furan-3-yl-(E)-acryloyl)- MS [M + 1]⁺: 615 amino]ethoxy}phenyl)propionic acid I_188 IIa_186 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.266 A {3-[benzyl-(3-furan-3-yl-(E)-acryloyl)- MS [M + 1]⁺: 629 amino]propoxy}phenyl)propionic acid I_189 IIa_187 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.303 A {2-[benzyl-(3-pyridin-3-yl-(E)-acryloyl)- MS [M + 1]⁺: 626 amino]ethoxy}phenyl)propionic acid I_190 IIa_188 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.428 A {3-[benzyl-(3-pyridin-3-yl-(E)-acryloyl)- MS [M + 1]⁺: 640 amino]propoxy}phenyl)propionic acid I_191 IIa_189 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.388 A {2-[benzyl-(3-thiophen-3-yl-(E)- MS [M + 1]⁺: 631 acryloyl)amino]ethoxy}phenyl)- propionic acid I_192 IIa_190 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.489 A {3-[benzyl-(3-thiophen-3-yl-(E)- MS [M + 1]⁺: 645 acryloyl)amino]propoxy}phenyl)- propionic acid I_193 IIa_191 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.008 A (benzylbut-2-(E)-enoylamino)ethoxy]- MS [M + 1]⁺: 563 phenyl}propionic acid I_194 IIa_192 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.114 A (benzylbut-2-(E)-enoylamino)- MS [M + 1]⁺: 577 propoxy]phenyl}propionic acid I_195 IIa_193 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.325 A {2-[benzyl-(2-thiophen-2-ylacetyl)- MS [M + 1]⁺: 619 amino]ethoxy}phenyl)propionic acid I_196 IIa_194 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.441 A {3-[benzyl-(2-thiophen-2-ylacetyl)- MS [M + 1]⁺: 633 amino]propoxy}phenyl)propionic acid I_197 IIa_195 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 6.546 A {2-[benzyl-(2-pyridin-3-ylacetyl)- MS [M + 1]⁺: 614 amino]ethoxy}phenyl)propionic acid I_198 IIa_196 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 6.683 A {3-[benzyl-(2-pyridin-3-ylacetyl)- MS [M + 1]⁺: 628 amino]propoxy}phenyl)propionic acid I_199 IIa_197 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.32 A {2-[benzyl-(2-thiophen-3-ylacetyl)- MS [M + 1]⁺: 619 amino]ethoxy}phenyl)propionic acid I_200 IIa_198 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.417 A {3-[benzyl-(2-thiophen-3-ylacetyl)- MS [M + 1]⁺: 633 amino]propoxy}phenyl)propionic acid I_201 IIa_199 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.803 A {2-[benzyl(3,3-dimethylbutyryl)amino]- MS [M + 1]⁺: 593 ethoxy}phenyl)propionic acid I_202 IIa_200 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.88 A {3-[benzyl(3,3-dimethylbutyryl)amino]- MS [M + 1]⁺: 607 propoxy}phenyl)propionic acid I_203 IIa_201 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.483 A {2-[benzyl-(3-methylbutyryl)amino]- MS [M + 1]⁺: 579 ethoxy}phenyl)propionic acid I_204 IIa_202 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.562 A {3-[benzyl-(3-methylbutyryl)amino]- MS [M + 1]⁺: 593 propoxy}phenyl)propionic acid I_205 IIa_203 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 6.329 A {2-[benzyl-(3-pyridin-3-ylpropionyl)- MS [M + 1]⁺: 628 amino]ethoxy}phenyl)propionic acid I_206 IIa_204 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 6.584 A {3-[benzyl-(3-pyridin-3-ylpropionyl)- MS [M + 1]⁺: 642 amino]propoxy}phenyl)propionic acid I_207 IIa_205 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.32 A (benzylpent-4-enoylamino)ethoxy]- MS [M + 1]⁺: 577 phenyl}propionic acid I_208 IIa_206 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.401 A (benzylpent-4-enoylamino)propoxy]- MS [M + 1]⁺: 591 phenyl}propionic acid I_209 IIa_207 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.628 A {2-[benzyl-(3-phenylpropionyl)amino]- MS [M + 1]⁺: 627 ethoxy}phenyl)propionic acid I_210 IIa_208 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.732 A {3-[benzyl-(3-phenylpropionyl)amino]- MS [M + 1]⁺: 641 propoxy}phenyl)propionic acid I_211 IIa_209 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.41 A (benzylcyclobutanecarbonylamino)- MS [M + 1]⁺: 577 ethoxy]phenyl}propionic acid I_212 IIa_210 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.481 A (benzylcyclobutanecarbonylamino)- MS [M + 1]⁺: 591 propoxy]phenyl}propionic acid I_213 IIa_211 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.786 A (benzylcyclohexanecarbonylamino)- MS [M + 1]⁺: 605 ethoxy]phenyl}propionic acid I_214 IIa_212 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.865 A (benzylcyclohexanecarbonylamino)- MS [M + 1]⁺: 619 propoxy]phenyl}propionic acid I_215 IIa_213 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.382 A {2-[benzyl-(3-cyclohexylpropionyl)- MS [M + 1]⁺: 633 amino]ethoxy}phenyl)propionic acid I_216 IIa_214 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.479 A {3-[benzyl-(3-cyclohexylpropionyl)- MS [M + 1]⁺: 647 amino]propoxy}phenyl)propionic acid I_217 IIa_215 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.109 A {2-[benzyl-(2-cyclohexylacetyl)amino]- MS [M + 1]⁺: 619 ethoxy}phenyl)propionic acid I_218 IIa_216 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.207 A {3-[benzyl-(2-cyclohexylacetyl)amino]- MS [M + 1]⁺: 633 propoxy}phenyl)propionic acid I_219 IIa_217 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.663 A (benzylcyclopentanecarbonylamino)- MS [M + 1]⁺: 591 ethoxy]phenyl}propionic acid I_220 IIa_218 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.84 A (benzylcyclopentanecarbonylamino)- MS [M + 1]⁺: 605 propoxy]phenyl}propionic acid I_221 IIa_219 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.16 A {2-[benzyl-(3-cyclopentylpropionyl)- MS [M + 1]⁺: 619 amino]ethoxy}phenyl)propionic acid I_222 IIa_220 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.208 A {3-[benzyl-(3-cyclopentylpropionyl)- MS [M + 1]⁺: 633 amino]propoxy}phenyl)propionic acid I_223 IIa_221 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.08 A (benzylcyclopropanecarbonylamino)- MS [M + 1]⁺: 563 ethoxy]phenyl}propionic acid I_224 IIa_222 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.181 A (benzylcyclopropanecarbonylamino)- MS [M + 1]⁺: 577 propoxy]phenyl}propionic acid I_225 IIa_223 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 7.968 A (benzylpropionylamino)ethoxy]- MS [M + 1]⁺: 551 phenyl}propionic acid I_226 IIa_224 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.054 A (benzylpropionylamino)propoxy]- MS [M + 1]⁺: 565 phenyl}propionic acid I_227 IIa_225 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.225 A (benzylisobutyrylamino)ethoxy]- MS [M + 1]⁺: 565 phenyl}propionic acid I_228 IIa_226 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.311 A (benzylisobutyrylamino)propoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid I_229 IIa_227 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.843 A (benzylhexanoylamino)ethoxy]- MS [M + 1]⁺: 593 phenyl}propionic acid I_230 IIa_228 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.898 A (benzylhexanoylamino)propoxy]- MS [M + 1]⁺: 607 phenyl}propionic acid I_231 IIa_229 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.507 A (benzylpentanoylamino)ethoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid I_232 IIa_230 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.581 A (benzylpentanoylamino)propoxy]- MS [M + 1]⁺: 593 phenyl}propionic acid I_233 IIa_231 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 9.396 A (benzyloctanoylamino)ethoxy]phenyl}- MS [M + 1]⁺: 621 propionic acid I_234 IIa_232 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 9.432 A (benzyloctanoylamino)propoxy]- MS [M + 1]⁺: 635 phenyl}propionic acid I_235 IIa_233 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 9.112 A (benzylheptanoylamino)ethoxy]- MS [M + 1]⁺: 607 phenyl}propionic acid I_236 IIa_234 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 9.158 A (benzylheptanoylamino)propoxy]- MS [M + 1]⁺: 621 phenyl}propionic acid I_237 IIa_235 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 9.653 A (benzylnonanoylamino)ethoxy]- MS [M + 1]⁺: 635 phenyl}propionic acid I_238 IIa_236 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 9.69 A (benzylnonanoylamino)propoxy]- MS [M + 1]⁺: 649 phenyl}propionic acid I_239 IIa_237 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.256 A (benzylbutyrylamino)ethoxy]phenyl}- MS [M + 1]⁺: 565 propionic acid I_240 IIa_238 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.332 A (benzylbutyrylamino)propoxy]phenyl}- MS [M + 1]⁺: 579 propionic acid I_241 IIa_239 (S)-3-{4-[2-(Benzoylbenzylamino)- rt: 8.333 A ethoxy]phenyl}-2-(2- MS [M + 1]⁺: 599 benzoylphenylamino)propionic acid I_242 IIa_240 (S)-3-{4-[3-(Benzoylbenzylamino)- rt: 8.378 A propoxy]phenyl}-2-(2- MS [M + 1]⁺: 613 benzoylphenylamino)propionic acid I_243 IIa_241 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.579 A {2-[benzyl-(3-phenylacryloyl)amino]- MS [M + 1]⁺: 625 ethoxy}phenyl)propionic acid I_244 IIa_242 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.68 A {3-[benzyl-(3-phenylacryloyl)amino]- MS [M + 1]⁺: 639 propoxy}phenyl)propionic acid I_245 IIa_243 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.628 A {2-[benzyl-(2,2-dimethylpropionyl)- MS [M + 1]⁺: 579 amino]ethoxy}phenyl)propionic acid I_246 IIa_244 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.656 A {3-[benzyl-(2,2-dimethylpropionyl)- MS [M + 1]⁺: 593 amino]propoxy}phenyl)propionic acid I_247 IIa_245 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.676 A {2-[cyclohexyl-(3-furan-2-ylacryloyl)- MS [M + 1]⁺: 607 amino]ethoxy}phenyl)propionic acid I_248 IIa_246 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.913 A (cyclobutanecarbonylcyclohexylamino) MS [M + 1]⁺: 569 ethoxy]phenyl}propionic acid I_249 IIa_247 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.607 A {2-[cyclohexyl-(3- MS [M + 1]⁺: 611 cyclopentylpropionyl)amino]ethoxy}- phenyl)propionic acid I_250 IIa_248 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.691 A (butyrylcyclohexylamino)ethoxy]- MS [M + 1]⁺: 557 phenyl}propionic acid I_251 IIa_249 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.536 A {2-[cyclopropylmethyl(naphthalene-2- MS [M + 1]⁺: 613 carbonyl)amino]ethoxy}phenyl)- propionic acid I_252 IIa_250 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.609 A {3-[cyclopropylmethyl(naphthalene-2- MS [M + 1]⁺: 627 carbonyl)amino]propoxy}phenyl)- propionic acid I_253 IIa_251 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.206 A {2-[cyclopropylmethyl(quinoline-2- MS [M + 1]⁺: 614 carbonyl)amino]ethoxy}phenyl)- propionic acid I_254 IIa_252 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.267 A {3-[cyclopropylmethyl(quinoline-2- MS [M + 1]⁺: 628 carbonyl)amino]propoxy}phenyl)- propionic acid I_255 IIa_253 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.084 A {2-[cyclopropylmethyl(quinoxaline-2- MS [M + 1]⁺: 615 carbonyl)amino]ethoxy}phenyl)- propionic acid I_256 IIa_254 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.192 A {3-[cyclopropylmethyl(quinoxaline-2- MS [M + 1]⁺: 629 carbonyl)amino]propoxy}phenyl)- propionic acid I_257 IIa_255 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.068 A {2-[cyclopropylmethyl(thiophene-2- MS [M + 1]⁺: 569 carbonyl)amino]ethoxy}phenyl)- propionic acid I_258 IIa_256 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.17 A {3-[cyclopropylmethyl(thiophene-2- MS [M + 1]⁺: 583 carbonyl)amino]propoxy}phenyl)- propionic acid I_259 IIa_257 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.1 A {2-[cyclopropylmethyl(pyridine-3- MS [M + 1]⁺: 564 carbonyl)amino]ethoxy}phenyl)- propionic acid I_260 IIa_258 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.229 A {3-[cyclopropylmethyl(pyridine-3- MS [M + 1]⁺: 578 carbonyl)amino]propoxy}phenyl)- propionic acid I_261 IIa_259 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.179 A (cyclopropylmethylphenylacetylamino) MS [M + 1]⁺: 577 ethoxy]phenyl}propionic acid I_262 IIa_260 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.268 A (cyclopropylmethylphenylacetylamino) MS [M + 1]⁺: 591 propoxy]phenyl}propionic acid I_263 IIa_261 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.056 A {2-[cyclopropylmethyl-(3-furan-2- MS [M + 1]⁺: 579 ylacryloyl)amino]ethoxy}phenyl)- propionic acid I_264 IIa_262 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.149 A {3-[cyclopropylmethyl-(3-furan-2- MS [M + 1]⁺: 593 ylacryloyl)amino]propoxy}phenyl)- propionic acid I_265 IIa_263 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.239 A {2-[cyclopropylmethyl-(3-thiophen-2- MS [M + 1]⁺: 595 ylacryloyl)amino]ethoxy}phenyl)- propionic acid I_266 IIa_264 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.342 A {3-[cyclopropylmethyl-(3-thiophen-2- MS [M + 1]⁺: 609 ylacryloyl)amino]propoxy}phenyl)- propionic acid I_267 IIa_265 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.085 A {2-[cyclopropylmethyl-(2-thiophen-2- MS [M + 1]⁺: 583 ylacetyl)amino]ethoxy}phenyl)- propionic acid I_268 IIa_266 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.175 A {3-[cyclopropylmethyl-(2-thiophen-2- MS [M + 1]⁺: 597 ylacetyl)amino]propoxy}phenyl)- propionic acid I_269 IIa_267 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.056 A {2-[cyclopropylmethyl-(2-thiophen-3- MS [M + 1]⁺: 583 ylacetyl)amino]ethoxy}phenyl)- propionic acid I_270 IIa_268 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.142 A {3-[cyclopropylmethyl-(2-thiophen-3- MS [M + 1]⁺: 597 ylacetyl)amino]propoxy}phenyl)- propionic acid I_271 IIa_269 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 6.234 A {2-[cyclopropylmethyl-(3-pyridin-3- MS [M + 1]⁺: 592 ylpropionyl)amino]ethoxy}phenyl)- propionic acid I_272 IIa_270 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 6.385 A {3-[cyclopropylmethyl-(3-pyridin-3- MS [M + 1]⁺: 606 ylpropionyl)amino]propoxy}phenyl)- propionic acid I_273 IIa_271 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.413 A {2-[cyclopropylmethyl-(3- MS [M + 1]⁺: 591 phenylpropionyl)amino]ethoxy}- phenyl)propionic acid I_274 IIa_272 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.488 A {3-[cyclopropylmethyl-(3- MS [M + 1]⁺: 605 phenylpropionyl)amino]propoxy}- phenyl)propionic acid I_275 IIa_273 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.16 A (cyclobutanecarbonylcyclopropylmethyl- MS [M + 1]⁺: 541 amino)ethoxy]phenyl}propionic acid I_276 IIa_274 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.24 A (cyclobutanecarbonylcyclopropylmethyl- MS [M + 1]⁺: 555 amino)propoxy]phenyl}propionic acid I_277 IIa_275 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.907 A {2-[(2-cyclohexylacetyl)- MS [M + 1]⁺: 583 cyclopropylmethylamino]ethoxy}- phenyl)propionic acid I_278 IIa_276 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.975 A {3-[(2-cyclohexylacetyl)- MS [M + 1]⁺: 597 cyclopropylmethylamino]propoxy}- phenyl)propionic acid I_279 IIa_277 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.405 A (cyclopentanecarbonylcyclopropylmethyl- MS [M + 1]⁺: 555 amino)ethoxy]phenyl}propionic acid I_280 IIa_278 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.486 A (cyclopentanecarbonylcyclopropylmethyl- MS [M + 1]⁺: 569 amino)propoxy]phenyl}propionic acid I_281 IIa_279 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 7.808 A (cyclopropanecarbonylcyclopropylmethyl- MS [M + 1]⁺: 527 amino)ethoxy]phenyl}propionic acid I_282 IIa_280 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 7.905 A (cyclopropanecarbonylcyclopropylmethyl- MS [M + 1]⁺: 541 amino)propoxy]phenyl}propionic acid I_283 IIa_281 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 7.682 A (cyclopropylmethylpropionylamino)- MS [M + 1]⁺: 515 ethoxy]phenyl}propionic acid I_284 IIa_282 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 7.776 A (cyclopropylmethylpropionylamino)- MS [M + 1]⁺: 529 propoxy]phenyl}propionic acid I_285 IIa_283 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 7.966 A (cyclopropylmethylisobutyrylamino)- MS [M + 1]⁺: 529 ethoxy]phenyl}propionic acid I_286 IIa_284 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.056 A (cyclopropylmethylisobutyrylamino)- MS [M + 1]⁺: 543 propoxy]phenyl}propionic acid I_287 IIa_285 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 7.99 A (butyrylcyclopropylmethylamino)- MS [M + 1]⁺: 529 ethoxy]phenyl}propionic acid I_288 IIa_286 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.071 A (butyrylcyclopropylmethylamino)- MS [M + 1]⁺: 543 propoxy]phenyl}propionic acid I_289 IIa_287 (S)-3-{4-[2- rt: 8.06 A (Benzoylcyclopropylmethylamino)- MS [M + 1]⁺: 563 ethoxy]phenyl}-2-(2- benzoylphenylamino)propionic acid I_290 IIa_288 (S)-3-{4-[3- rt: 8.161 A (Benzoylcyclopropylmethylamino)- MS [M + 1]⁺: 577 propoxy]phenyl}-2-(2- benzoylphenylamino)propionic acid I_291 IIa_289 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.338 A {2-[cyclopropylmethyl-(3- MS [M + 1]⁺: 589 phenylacryloyl)amino]ethoxy}phenyl)- propionic acid I_292 IIa_290 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.424 A {3-[cyclopropylmethyl-(3- MS [M + 1]⁺: 603 phenylacryloyl)amino]propoxy}- phenyl)propionic acid I_293 IIa_291 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.404 A {2-[(naphthalene-1-carbonyl)- MS [M + 1]⁺: 635 phenylamino]ethoxy}phenyl)propionic acid I_294 IIa_292 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.588 A {3-[(naphthalene-1-carbonyl)- MS [M + 1]⁺: 649 phenylamino]propoxy}phenyl)- propionic acid I_295 IIa_293 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.618 A {2-[(naphthalene-2-carbonyl)- MS [M + 1]⁺: 635 phenylamino]ethoxy}phenyl)propionic acid I_296 IIa_294 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.762 A {3-[(naphthalene-2-carbonyl)- MS [M + 1]⁺: 649 phenylamino]propoxy}phenyl)- propionic acid I_297 IIa_295 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.095 A {2-[(quinoline-2-carbonyl)- MS [M + 1]⁺: 636 phenylamino]ethoxy}phenyl)propionic acid I_298 IIa_296 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.241 A {3-[phenyl(quinoline-2-carbonyl)- MS [M + 1]⁺: 650 amino]propoxy}phenyl)propionic acid I_299 IIa_297 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: _(—) A {2-[phenyl(quinoxaline-2-carbonyl)- MS [M + 1]⁺: 637 amino]ethoxy}phenyl)propionic acid I_300 IIa_298 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.214 A {3-[phenyl(quinoxaline-2-carbonyl)- MS [M + 1]⁺: 651 amino]propoxy}phenyl)propionic acid I_301 IIa_299 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.259 A {2-[phenyl(thiophene-2-carbonyl)- MS [M + 1]⁺: 591 amino]ethoxy}phenyl)propionic acid I_302 IIa_300 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.416 A {3-[phenyl(thiophene-2-carbonyl)- MS [M + 1]⁺: 605 amino]propoxy}phenyl)propionic acid I_303 IIa_301 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.925 A {2-[(isoquinoline-3-carbonyl)- MS [M + 1]⁺: 636 phenylamino]ethoxy}phenyl)propionic acid I_304 IIa_302 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.253 A {2-[phenyl(pyridine-3-carbonyl)amino]- MS [M + 1]⁺: 586 ethoxy}phenyl)propionic acid I_305 IIa_303 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.434 A {3-[phenyl(pyridine-3-carbonyl)amino]- MS [M + 1]⁺: 600 propoxy}phenyl)propionic acid I_306 IIa_304 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.061 A {2-[phenyl(pyridine-4-carbonyl)amino]- MS [M + 1]⁺: 586 ethoxy}phenyl)propionic acid I_307 IIa_305 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.261 A {3-[phenyl(pyridine-4-carbonyl)amino]- MS [M + 1]⁺: 600 propoxy}phenyl)propionic acid I_308 IIa_306 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.439 A (phenylphenylacetylamino)ethoxy]- MS [M + 1]⁺: 599 phenyl}propionic acid I_309 IIa_307 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.619 A (phenylphenylacetylamino)propoxy]- MS [M + 1]⁺: 613 phenyl}propionic acid I_310 IIa_308 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.98 A {2-[(2-methylacryloyl)phenylamino]- MS [M + 1]⁺: 549 ethoxy}phenyl)propionic acid I_311 IIa_309 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.146 A {2-[(2-methylacryloyl)phenylamino]- MS [M + 1]⁺: 563 propoxy}phenyl)propionic acid I_312 IIa_310 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.511 A {2-[phenyl-(3-phenylpropynoyl)amino]- MS [M + 1]⁺: 609 ethoxy}phenyl)propionic acid I_313 IIa_311 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.759 A {2-[(2-ethylbutyryl)phenylamino]- MS [M + 1]⁺: 579 ethoxy}phenyl)propionic acid I_314 IIa_312 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.917 A {3-[(2-ethylbutyryl)phenylamino]- MS [M + 1]⁺: 593 propoxy}phenyl)propionic acid I_315 IIa_313 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.259 A {2-[(3-furan-2-ylacryloyl)phenylamino]- MS [M + 1]⁺: 601 ethoxy}phenyl)propionic acid I_316 IIa_314 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.422 A {3-[(3-furan-2-ylacryloyl)phenylamino]- MS [M + 1]⁺: 615 propoxy}phenyl)propionic acid I_317 IIa_315 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.521 A {2-[phenyl-(3-thiophen-2-ylacryloyl)- MS [M + 1]⁺: 617 amino]ethoxy}phenyl)propionic acid I_318 IIa_316 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.677 A {3-[phenyl-(3-thiophen-2-ylacryloyl)- MS [M + 1]⁺: 631 amino]propoxy}phenyl)propionic acid I_319 IIa_317 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.191 A {2-[(3-furan-3-yl-(E)-acryloyl)- MS [M + 1]⁺: 601 phenylamino]ethoxy}phenyl)propionic acid I_320 IIa_318 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.348 A {3-[(3-furan-3-yl-(E)-acryloyl)- MS [M + 1]⁺: 615 phenylamino]propoxy}phenyl)- propionic acid I_321 IIa_319 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.217 A {2-[phenyl-(3-pyridin-3-yl-(E)-acryloyl)- MS [M + 1]⁺: 612 amino]ethoxy}phenyl)propionic acid I_322 IIa_320 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.417 A {3-[phenyl-(3-pyridin-3-yl-(E)-acryloyl)- MS [M + 1]⁺: 626 amino]propoxy}phenyl)propionic acid I_323 IIa_321 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.471 A {2-[phenyl-(3-thiophen-3-yl-(E)- MS [M + 1]⁺: 617 acryloyl)amino]ethoxy}phenyl)- propionic acid I_324 IIa_322 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.616 A {3-[phenyl-(3-thiophen-3-yl-(E)- MS [M + 1]⁺: 631 acryloyl)amino]propoxy}phenyl)- propionic acid I_325 IIa_323 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.213 A (but-2-(E)-enoylphenylamino)- MS [M + 1]⁺: 563 propoxy]phenyl}propionic acid I_326 IIa_324 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.348 A {2-[phenyl-(2-thiophen-2-ylacetyl)- MS [M + 1]⁺: _(—) amino]ethoxy}phenyl)propionic acid I_327 IIa_325 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.506 A {3-[phenyl-(2-thiophen-2-ylacetyl)- MS [M + 1]⁺: 619 amino]propoxy}phenyl)propionic acid I_328 IIa_326 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.478 A {3-[phenyl-(2-thiophen-3-ylacetyl)- MS [M + 1]⁺: 619 amino]propoxy}phenyl)propionic acid I_329 IIa_327 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.882 A {2-[(3,3-dimethylbutyryl)phenylamino]- MS [M + 1]⁺: 579 ethoxy}phenyl)propionic acid I_330 IIa_328 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.037 A {3-[(3,3-dimethylbutyryl)phenylamino]- MS [M + 1]⁺: 593 propoxy}phenyl)propionic acid I_331 IIa_329 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.503 A {2-[(3-methylbutyryl)phenylamino]- MS [M + 1]⁺: 565 ethoxy}phenyl)propionic acid I_332 IIa_330 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.663 A {3-[(3-methylbutyryl)phenylamino]- MS [M + 1]⁺: 579 propoxy}phenyl)propionic acid I_333 IIa_331 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 6.373 A {2-[phenyl-(3-pyridin-3-ylpropionyl)- MS [M + 1]⁺: 614 amino]ethoxy}phenyl)propionic acid I_334 IIa_332 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 6.561 A {3-[phenyl-(3-pyridin-3-ylpropionyl)- MS [M + 1]⁺: 628 amino]propoxy}phenyl)propionic acid I_335 IIa_333 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.317 A (pent-4-enoylphenylamino)ethoxy]- MS [M + 1]⁺: 563 phenyl}propionic acid I_336 IIa_334 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.482 A (pent-4-enoylphenylamino)propoxy]- MS [M + 1]⁺: 577 phenyl}propionic acid I_337 IIa_335 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.631 A {2-[phenyl-(3-phenylpropionyl)amino]- MS [M + 1]⁺: 613 ethoxy}phenyl)propionic acid I_338 IIa_336 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.791 A {3-[phenyl-(3-phenylpropionyl)amino]- MS [M + 1]⁺: 627 propoxy}phenyl)propionic acid I_339 IIa_337 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.432 A (cyclobutanecarbonylphenylamino)- MS [M + 1]⁺: 563 ethoxy]phenyl}propionic acid I_340 IIa_338 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.594 A (cyclobutanecarbonylphenylamino)- MS [M + 1]⁺: 577 propoxy]phenyl}propionic acid I_341 IIa_339 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: _(—) A (cyclohexanecarbonylphenylamino)- MS [M + 1]⁺: _(—) ethoxy]phenyl}propionic acid I_342 IIa_340 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.986 A (cyclohexanecarbonylphenylamino)- MS [M + 1]⁺: 605 propoxy]phenyl}propionic acid I_343 IIa_341 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.466 A {2-[(3-cyclohexylpropionyl)- MS [M + 1]⁺: 619 phenylamino]ethoxy}phenyl)propionic acid I_344 IIa_342 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.587 A {3-[(3-cyclohexylpropionyl)- MS [M + 1]⁺: 633 phenylamino]propoxy}phenyl)- propionic acid I_345 IIa_343 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.175 A {2-[(2-cyclohexylacetyl)phenylamino]- MS [M + 1]⁺: 605 ethoxy}phenyl)propionic I_346 IIa_344 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.316 A {3-[(2-cyclohexylacetyl)phenylamino]- MS [M + 1]⁺: 619 propoxy}phenyl)propionic acid I_347 IIa_345 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.68 A (cyclopentanecarbonylphenylamino)- MS [M + 1]⁺: 577 ethoxy]phenyl}propionic acid I_348 IIa_346 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.839 A (cyclopentanecarbonylphenylamino)- MS [M + 1]⁺: 591 propoxy]phenyl}propionic acid I_349 IIa_347 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.207 A {2-[(3-cyclopentylpropionyl)- MS [M + 1]⁺: 605 phenylamino]ethoxy}phenyl)propionic acid I_350 IIa_348 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.339 A {3-[(3-cyclopentylpropionyl)- MS [M + 1]⁺: 619 phenylamino]propoxy}phenyl)- propionic acid I_351 IIa_349 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.11 A (cyclopropanecarbonylphenylamino)- MS [M + 1]⁺: 549 ethoxy]phenyl}propionic acid I_352 IIa_350 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.284 A (cyclopropanecarbonylphenylamino)- MS [M + 1]⁺: 563 propoxy]phenyl}propionic acid I_353 IIa_351 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 7.965 A (phenylpropionylamino)ethoxy]- MS [M + 1]⁺: 537 phenyl}propionic acid I_354 IIa_352 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.138 A (phenylpropionylamino)propoxy]- MS [M + 1]⁺: 551 phenyl}propionic acid I_355 IIa_353 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.246 A (isobutyrylphenylamino)ethoxy]- MS [M + 1]⁺: 551 phenyl}propionic acid I_356 IIa_354 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.411 A (isobutyrylphenylamino)propoxy]- MS [M + 1]⁺: 656 phenyl}propionic acid I_357 IIa_355 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.850 A (hexanoylphenylamino)ethoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid I_358 IIa_356 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.996 A (hexanoylphenylamino)propoxy]- MS [M + 1]⁺: 593 phenyl}propionic acid I_359 IIa_357 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.535 A (pentanoylphenylamino)ethoxy]- MS [M + 1]⁺: 565 phenyl}propionic acid I_360 IIa_358 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.691 A (pentanoylphenylamino)propoxy]- MS [M + 1]⁺: 579 phenyl}propionic acid I_361 IIa_359 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 9.465 A (octanoylphenylamino)ethoxy]phenyl}- MS [M + 1]⁺: 607 propionic acid I_362 IIa_360 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 9.587 A (octanoylphenylamino)propoxy]- MS [M + 1]⁺: 621 phenyl}propionic acid I_363 IIa_361 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 9.168 A (heptanoylphenylamino)ethoxy]- MS [M + 1]⁺: 593 phenyl}propionic acid I_364 IIa_362 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 9.302 A (heptanoylphenylamino)propoxy]- MS [M + 1]⁺: 607 phenyl}propionic acid I_365 IIa_363 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 9.736 A (nonanoylphenylamino)ethoxy]- MS [M + 1]⁺: 621 phenyl}propionic acid I_366 IIa_364 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 9.85 A (nonanoylphenylamino)propoxy]- MS [M + 1]⁺: 635 phenyl}propionic acid I_367 IIa_365 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.259 A (butyrylphenylamino)ethoxy]phenyl}- MS [M + 1]⁺: 551 propionic acid I_368 IIa_366 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.426 A (butyrylphenylamino)propoxy]phenyl}- MS [M + 1]⁺: 565 propionic acid I_369 IIa_367 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.172 A (benzoylphenylamino)ethoxy]phenyl}- MS [M + 1]⁺: 585 propionic acid I_370 IIa_368 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.348 A (benzoylphenylamino)propoxy]- MS [M + 1]⁺: 599 phenyl}propionic acid I_371 IIa_369 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.647 A {2-[phenyl-(3-phenylacryloyl)amino]- MS [M + 1]⁺: 611 ethoxy}phenyl)propionic acid I_372 IIa_370 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.81 A {3-[phenyl-(3-phenylacryloyl)amino]- MS [M + 1]⁺: 625 propoxy}phenyl)propionic acid I_373 IIa_371 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.661 A {2-[(2,2-dimethylpropionyl)- MS [M + 1]⁺: 565 phenylamino]ethoxy}phenyl)propionic acid I_374 IIa_372 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.79 A {3-[(2,2-dimethylpropionyl)- MS [M + 1]⁺: 579 phenylamino]propoxy}phenyl)- propionic acid I_375 IIa_373 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.443 A (tert-butylcyclobutanecarbonylamino)- MS [M + 1]⁺: 543 ethoxy]phenyl}propionic acid I_376 IIa_374 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.194 A {2-[tert-butyl-(3-cyclopentylpropionyl)- MS [M + 1]⁺: 585 amino]ethoxy}phenyl)propionic acid I_377 II_1 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- 8.98 (bs, 1H), 7.56 (d, A (benzylindan-5-ylamino)ethoxy]- 2H), 7.45-7.37 (ca, 5H), phenyl}propionic acid 7.27-7.19 (ca, 8H), 7.01 (t, 1H), 6.71-6.65 (ca, 3H), 6.54-6.41 (ca, 2H), 4.60 (s, 2H), 4.27 (m, 1H), 4.07 (t, 2H), 3.76 (t, 2H), 3.27 (dd, 1H), 3.08 (m, 1H), 2.80 (ca, 4H), 2.01 (ca, 2H) I_378 II_2 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.342 A {2-[benzyl(2,6-difluorophenyl)amino]- MS [M + 1]⁺: 607 ethoxy}phenyl)propionic acid I_379 II_3 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.516 A {2-[(2-chlorophenyl)-(2-fluorobenzyl)- MS [M + 1]⁺: 624 amino]ethoxy}phenyl)propionic acid I_380 II_4 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.98 (bs, 1H), 7.56 (d, A {2-[benzyl-(2-fluorophenyl)amino]- 2H), 7.46-7.37 (ca, 5H), ethoxy}phenyl)propionic acid 7.32-7.18 (m, 9H), 6.98-6.91 (ca, 2H), 6.70-6.65 (ca, 3H), 6.44 (t, 1H), 4.46 (s, 2H), 4.27 (m, 1H), 3.99 (t, 2H), 3.56 (t, 2H), 3.27 (m, 1H), 3.08 (m, 1H) I_381 II_5 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.88 (bs, 1H), 7.57 (d, A {2-[(2-methylbenzyl)phenylamino]- 2H), 7.55-7.32 (ca, 6H), ethoxy}phenyl)propionic acid 7.24-7.09 (ca, 8H), 6.75-6.64 (ca, 5H), 6.58 (t, 1H), 4.55 (s, 2H), 4.33 (m, 1H), 4.11 (t, 2H), 3.80 (t, 2H), 3.25 (m, 1H), 3.09 (m, 1H), 2.34 (s, 3H) I_382 II_6 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.546 A {2-[(3-chlorophenyl)-(2- MS [M + 1]⁺: 636 methoxybenzyl)amino]ethoxy}phenyl)- propionic acid I_383 II_7 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.461 A {2-[(2-methoxybenzyl)-m-tolylamino]- MS [M + 1]⁺: 615 ethoxy}phenyl)propionic acid I_384 II_8 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.292 A {3-[(2-methoxybenzyl)phenylamino]- MS [M + 1]⁺: 615 propoxy}phenyl)propionic acid I_385 II_9 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 9.523 A (benzyl-o-tolylamino)ethoxy]phenyl}- MS [M + 1]⁺: 585 propionic acid I_386 II_10 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.98 (bs, 1H), 7.56 (d, A {2-[benzyl-(3-ethylphenyl)amino]- 2H), 7.45-7.37 (ca, 5H), ethoxy}phenyl)propionic acid 7.28-7.20 (m, 9H), 7.08 (t, 1H), 6.70 (d, 2H), 6.58-6.52 (ca, 2H), 6.43 (t, 1H), 4.62 (s, 2H), 4.27 (m, 1H), 4.09 (t, 2H), 3.78 (t, 2H), 3.27 (m, 1H), 3.08 (m, 1H), 2.53 (q, 2H), 1.14 (t, 3H) I_387 II_11 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.98 (bs, 1H), 7.56 (d, A {2-[benzyl-(3-fluorophenyl)amino]- 2H), 7.46-7.37 (ca, 5H), ethoxy}phenyl)propionic acid 7.31-7.17 (ca, 8H), 7.08 (m, 1H), 6.70 (ca, 3H), 6.48-6.32 (ca, 3H), 4.62 (s, 2H), 4.27 (m, 1H), 4.08 (t, 2H), 3.78 (t, 2H), 3.27 (dd, 1H), 3.08 (m, 1H) I_388 II_12 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.428 A {2-[(2-chlorophenyl)-(3- MS [M + 1]⁺: 636 methoxybenzyl)amino]ethoxy}phenyl)- propionic acid I_389 II_13 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.375 A {2-[(3-chlorophenyl)-(3- MS [M + 1]⁺: 636 methoxybenzyl)amino]ethoxy}phenyl)- propionic acid I_390 II_14 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.354 A {2-[(3-methoxybenzyl)-m-tolylamino]- MS [M + 1]⁺: 615 ethoxy}phenyl)propionic acid I_391 II_15 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.259 A {3-[(3-methoxybenzyl)phenylamino]- MS [M + 1]⁺: 615 propoxy}phenyl)propionic acid I_392 II_16 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- 8.98 (bs, 1H), 7.56 (d, A (benzyl-m-tolylamino)ethoxy]phenyl}- 2H), 7.45-7.37 (ca, 5H), propionic acid 7.27-7.19 (ca, 7H), 7.05 (t, 1H), 6.71-6.68 (ca, 3H), 6.56-6.42 (ca, 4H), 4.61 (s, 2H), 4.28 (m, 1H), 4.07 (t, 2H), 3.77 (t, 2H), 3.26 (dd, 1H), 3.06 (m, 1H), 2.25 (s, 3H) I_393 II_17 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.98 (bs, 1H), 7.56 (d, A {2-[benzyl-(4-chlorophenyl)amino]- 2H), 7.47-7.39 (ca, 5H), ethoxy}phenyl)propionic acid 7.30-7.16 (ca, 8H), 7.08 (d, 2H), 6.72-6.61 (ca, 4H), 6.44 (t, 1H), 4.60 (s, 2H), 4.27 (m, 1H), 4.07 (t, 2H), 3.77 (t, 2H), 3.26 (dd, 1H), 3.08 (m, 1H) I_394 II_18 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.98 (bs, 1H), 7.56 (d, A {2-[benzyl-(4-fluorophenyl)amino]- 2H), 7.46-7.37 (ca, 5H), ethoxy}phenyl)propionic acid 7.32-7.19 (ca, 8H), 6.89-6.84 (ca, 2H), 6.72-6.61 (ca, 4H), 6.44 (t, 1H), 4.57 (s, 2H), 4.28 (m, 1H), 4.06 (t, 2H), 3.75 (t, 2H), 3.27 (dd, 1H), 3.08 (m, 1H) I_395 II_19 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.96 (bs, 1H), 7.55 (d, A {2-[(4-methylbenzyl)phenylamino]- 2H), 7.46-7.37 (ca, 5H), ethoxy}phenyl)propionic acid 7.24-7.09 (m, 9H), 6.72-6.64 (ca, 5H), 6.45 (t, 1H), 4.58 (s, 2H), 4.27 (m, 1H), 4.06 (t, 2H), 3.77 (t, 2H), 3.27 (dd, 1H), 3.08 (m, 1H), 2.30 (s, 3H) I_396 II_20 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.178 A {3-[(4-methoxybenzyl)phenylamino]- MS [M + 1]⁺: 615 propoxy}phenyl)propionic acid I_397 II_21 (S)-2-(Benzoylphenylamino)-3-{4-[2- 8.96 (bs, 1H), 7.53 (d, A (di-p-tolylamino)ethoxy]phenyl}- 2H), 7.48-7.35 (ca, 5H), propionic acid 7.22-7.15 (m, 9H), 7.03 (d, 1H), 6.89 (d, 1H), 6.69-6.65 (ca, 3H), 6.43 (t, 1H), 4.23 (m, 1H), 4.02 (bs, 4H), 3.25 (m, 1H), 3.05 (m, 1H), 2.27 (s, 6H).. I_398 II_22 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- 8.83 (bs, 1H), A (benzyl-p-tolylamino)ethoxy]phenyl}- 7.50-6.93 (ca, 17H), propionic acid 6.60-6.55 (ca, 4H), 6.34 (t, 1H), 4.53 (s, 2H), 4.21 (m, 1H), 3.93 (t, 2H), 3.62 (t, 2H), 3.17 (dd, 1H), 2.98 (m, 1H), 2.19 (s, 3H) I_399 II_23 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 9.736 A (benzylindan-5-ylamino)propoxy]- MS [M + 1]⁺: 625 phenyl}propionic acid I_400 II_24 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.747 A {3-[benzyl-(3-ethylphenyl)amino]- MS [M + 1]⁺: 613 propoxy}phenyl)propionic acid I_401 II_25 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 9.549 A (benzyl-m-tolylamino)propoxy]- MS [M + 1]⁺: 599 phenyl}propionic acid I_402 II_26 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 9.526 A (benzyl-p-tolylamino)propoxy]phenyl}- MS [M + 1]⁺: 599 propionic acid I_403 II_27 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 6.67 A (benzylcyclohexylamino)propoxy]- MS [M + 1]⁺: 591 phenyl}propionic acid methyl ester I_404 II_28 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- 8.92 (bs, 1H), 7.56 (d, A (benzyphenylamino)propoxy]phenyl}- 2H), 7.46-7.37 (ca, 5H), propionic acid 7.30-7.10 (ca, 10H), 6.76-6.61 (ca, 5H), 6.44 (t, 1H), 4.53 (s, 2H), 4.28 (m, 1H), 3.92 (t, 2H), 3.62 (t, 2H), 3.22 (dd, 1H), 3.10 (m, 1H), 2.09-1.98 (ca, 2H) I_405 II_29 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.565 A {2-[(2-fluorophenyl)isobutylamino]- MS [M + 1]⁺: 555 ethoxy}phenyl)propionic acid I_406 II_30 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 9.729 A (isobutyl-o-tolylamino)ethoxy]phenyl}- MS [M + 1]⁺: 551 propionic acid I_407 II_31 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 9.443 A (isobutyl-o-tolylamino)propoxy]- MS [M + 1]⁺: 565 phenyl}propionic acid I_408 II_32 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.445 A {2-[(3-fluorophenyl)isobutylamino]- MS [M + 1]⁺: 555 ethoxy}phenyl)propionic acid I_409 II_33 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.65 A {2-[isobutyl-m-tolylamino]ethoxy}- MS [M + 1]⁺: 551 phenyl)propionic acid I_410 II_34 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.573 A {3-[isobutyl-m-tolylamino]propoxy}- MS [M + 1]⁺: 565 phenyl)propionic acid I_411 II_35 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- 8.99 (bs, 1H), 7.57 (d, A (benzylphenethylamino)ethoxy]- 2H), 7.46-7.36 (ca, 4H), phenyl}propionic acid 7.32-7.21 (ca, 11H), 7.13 (d, 2H), 6.73-6.69 (ca, 3H), 6.44 (t, 1H), 4.23 (m, 1H), 3.94 (t, 2H), 3.76 (s, 2H), 3.27 (m, 1H), 3.07 (m, 1H), 2.93 (t, 2H), 2.81 (bs, 4H) I_412 II_36 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 9.089 A (cyclobutylmethyl-o-tolylamino)- MS [M + 1]⁺: 563 ethoxy]phenyl}propionic acid I_413 II_37 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 6.418 A (benzylcyclopentylamino)ethoxy]- MS [M + 1]⁺: 563 phenyl}propionic acid I_414 II_38 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 6.97 A (cyclopentylphenylamino)propoxy]- MS [M + 1]⁺: 563 phenyl}propionic acid I_415 II_39 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.937 A {2-[cyclopentylmethyl-(2- MS [M + 1]⁺: 581 fluorophenyl)amino]ethoxy}phenyl)- propionic acid I_416 II_40 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- 8.84 (bs, 1H), A (cyclopentylmethylphenylamino)- 7.57-7.41 (ca, 7H), 7.22-7.16 (ca, ethoxy]phenyl}propionic acid 4H), 6.75-6.55 (ca, 7H), 4.31 (ca, 3H), 3.98 (t, 1H), 3.71 (t, 2H), 3.30-3.20 (ca, 3H), 3.09 (m, 1H), 2.29 (m, 1H), 1.75-1.54 (ca, 8H) I_417 II_41 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 6.432 A (benzylcyclopropylmethylamino)- MS [M + 1]⁺: 549 ethoxy]phenyl}propionic acid I_418 II_42 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 6.47 A (benzylcyclopropylmethylamino)- MS [M + 1]⁺: 563 propoxy]phenyl}propionic acid I_419 II_43 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.98 (bs, 1H), 7.57 (d, A {2-[(2-methoxybenzyl)phenylamino]- 2H), 7.48-7.39 (ca, 5H), ethoxy}phenyl)propionic acid 7.27-7.13 (ca, 6H), 7.05 (d, 1H), 6.88-6.80 (ca, 2H), 6.73-6.60 (ca, 5H), 6.44 (t, 1H), 4.59 (s, 2H), 4.27 (m, 1H), 4.10 (t, 2H), 3.85 (s, 3H), 3.79 (t, 2H), 3.27 (dd, 1H), 3.08 (m, 1H) I_420 II_44 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.98 (bs, 1H), 7.57 (d, A {2-[(3-methoxybenzyl)phenylamino]- 2H), 7.48-7.39 (ca, 5H), ethoxy}phenyl)propionic acid 7.27-7.13 (ca, 6H), 6.85-6.62 (ca, 8H), 6.44 (t, 1H), 4.60 (s, 2H), 4.27 (m, 1H), 4.10 (t, 2H), 3.85 (s, 3H), 3.79 (t, 2H), 3.27 (m, 1H), 3.08 (m, 1H) I_421 II_45 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.97 (bs, 1H), A {2-[(3-methoxyphenyl)phenylamino]- 7.55-7.35 (ca, 6H), 7.28-6.95 (ca, ethoxy}phenyl)propionic acid 11H), 6.68-6.40 (ca, 5H), 4.23 (m, 1H), 4.05 (bs, 4H), 3.71 (s, 3H), 3.25 (m, 1H), 3.05 (m, 1H) I_422 II_46 (S)-2-(2-Benzoylphenylamino)-3-(4- 8.98 (bs, 1H), 7.57 (d, A {2-[(4-methoxybenzyl)phenylamino]- 2H), 7.48-7.39 (ca, 5H), ethoxy}phenyl)propionic acid 7.27-7.13 (ca, 7H), 6.85 (d, 2H), 6.75-6.60 (ca, 5H), 6.42 (t, 1H), 4.59 (s, 2H), 4.27 (m, 1H), 4.10 (t, 2H), 3.79 (ca, 2H), 3.76 (s, 3H), 3.27 (m, 1H), 3.08 (m, 1H) I_423 II_47 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.939 A {2-[(4-tert-butylbenzyl)phenylamino]- MS [M + 1]⁺: 627 ethoxy}phenyl)propionic acid I_424 II_48 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- 8.70 (d, 1H), A (benzylphenylamino)ethoxy]phenyl}- 7.60-7.40 (ca, 4H), 7.40-7.10 (m, propionic acid 9H), 7.10-7.00 (ca, 4H), 6.80-6.60 (ca, 4H), 7.60-7.45 (ca, 2H), 4.60 (s, 2H), 4.31 (bs, 1H), 4.07 (t, 2H), 3.77 (t, 2H), 3.13 (dd, 1H), 2.96 (dd, 1H). I_425 II_49 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- 8.98 (d, 1H), 7.56 (d, A (cyclobutylmethylphenylamino)- 2H), 7.46-7.38 (ca, 4H), ethoxy]phenyl}propionic acid 7.21-7.15 (ca, 5H), 6.73-6.63 (ca, 6H), 6.45 (t, 1H), 4.27 (m, 1H), 3.97 (t, 2H), 3.68 (t, 2H), 3.37 (d, 2H), 3.26 (dd, 1H), 2.68 (m, 1H), 2.03-1.70 (ca, 6H) I_426 II_50 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 9.029 A (cyclohexylphenylamino)ethoxy]- MS [M + 1]⁺: 563 phenyl}propionic acid I_427 II_51 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- 8.98 (d, 1H), 7.57 (d, A (cyclohexylmethylphenylamino)- 2H), 7.46-7.38 (ca, 4H), ethoxy]phenyl}propionic acid 7.21-7.15 (ca, 6H), 6.67-6.63 (ca, 5H), 6.44 (t, 1H), 4.27 (m, 1H), 3.98 (t, 2H), 3.70 (t, 2H), 3.26 (dd, 1H), 3.17 (d, 2H), 3.06 (m, 1H), 1.80-1.50 (ca, 11H) I_428 II_52 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 7.669 A (cyclopentylphenylamino)ethoxy]- MS [M + 1]⁺: 549 phenyl}propionic acid I_429 II_53 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- 8.98 (bs, 1H), 7.56 (d, A (cyclopropylmethylphenylamino)- 2H), 7.44-7.40 (ca, 4H), ethoxy]phenyl}propionic acid 7.23-7.18 (ca, 6H), 6.78-6.66 (ca, 5H), 6.44 (t, 1H), 4.27 (m, 1H), 4.04 (t, 2H), 3.76 (t, 2H), 3.29-3.24 (ca, 3H), 3.06 (m, 1H), 1.00-0.80 (m, 1H), 0.54-0.40 (ca, 2H), 0.26-0.21 (ca, 2H) I_430 II_54 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- 8.62 (d, 1H), A (diphenylamino)ethoxy]phenyl}- 7.60-7.44 (ca, 4H), 7.38 (t, 1H), propionic acid 7.32 (dd, 2H), 7.24 (td, 4H), 7.07 (d, 2H), 6.99 (d, 4H), 6.91 (t, 2H), 6.82 (d, 1H), 6.73 (d, 2H), 6.57 (t, 1H), 4.50 (m, 1H), 4.05 (s, 4H), 3.25-2.95 (ca, 2H). I_431 IIa_375 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.502 A {2-[(2-methylacryloyl)naphthalen-1- MS [M + 1]⁺: 599 ylamino]ethoxy}phenyl)propionic acid I_432 IIa_376 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.432 A (but-2-(E)-enoylnaphthalen-1- MS [M + 1]⁺: 599 ylamino)ethoxy]phenyl}propionic acid I_433 IIa_377 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.485 A (cyclopropanecarbonylnaphthalen-1- MS [M + 1]⁺: 587 ylamino)ethoxy]phenyl}propionic acid I_434 IIa_378 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.563 A (naphthalen-1-ylpropionylamino)- MS [M + 1]⁺: 599 ethoxy]phenyl}propionic acid I_435 IIa_379 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.599 A {2-[(2-methylacryloyl)naphthalen-2- MS [M + 1]⁺: 599 ylamino]ethoxy}phenyl)propionic acid I_436 IIa_380 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.491 A (but-2-(E)-enoylnaphthalen-2- MS [M + 1]⁺: 599 ylamino)ethoxy]phenyl}propionic acid I_437 IIa_381 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.494 A (naphthalen-2-ylpropionylamino)- MS [M + 1]⁺: 587 ethoxy]phenyl}propionic acid I_438 IIa_382 (S)-3-{4-[2-(Acetylnaphthalen-2- rt: 8.099 A ylamino)ethoxy]phenyl}-2-(2- MS [M + 1]⁺: 573 benzoylphenylamino)propionic acid I_439 IIa_383 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.343 A {2-[(2-methylacryloyl)-(3- MS [M + 1]⁺: 595 methylsulfanylphenyl)amino]ethoxy}- phenyl)propionic acid I_440 IIa_384 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.261 A {2-[but-2-(E)-enoyl-(3- MS [M + 1]⁺: 595 methylsulfanylphenyl)amino]ethoxy}- phenyl)propionic acid I_441 IIa_385 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.51 A {2-[butyryl-(3-methylsulfanylphenyl)- MS [M + 1]⁺: 597 amino]ethoxy}phenyl)propionic acid I_442 IIa_386 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.36 A {2-[(2-methylacryloyl)-(4- MS [M + 1]⁺: 595 methylsulfanylphenyl)amino]ethoxy}- phenyl)propionic acid I_443 IIa_387 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.262 A {2-[but-2-(E)-enoyl-(4- MS [M + 1]⁺: 595 methylsulfanylphenyl)amino]ethoxy}- phenyl)propionic acid I_444 IIa_388 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.519 A {2-[isobutyryl-(4- MS [M + 1]⁺: 597 methylsulfanylphenyl)amino]ethoxy}- phenyl)propionic acid I_445 IIa_389 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.522 A {2-[butyryl-(4-methylsulfanylphenyl)- MS [M + 1]⁺: 597 amino]ethoxy}phenyl)propionic acid I_446 IIa_390 (S)-3-{4-[2-(Acetylnaphthalen-1- rt: 8.599 A ylamino)ethoxy]phenyl}-2-(2- MS [M + 1]⁺: _(—) benzoylphenylamino)propionic acid I_447 IIa_391 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.627 A (cyclopropanecarbonylnaphthalen-2- MS [M + 1]⁺: _(—) ylamino)ethoxy]phenyl}propionic acid I_448 IIa_392 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.464 A {3-[butyryl-(2-fluorophenyl)amino]- MS [M + 1]⁺: 583 propoxy}phenyl)propionic acid I_449 IIa_393 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.603 A {3-[cyclobutanecarbonyl-(2- MS [M + 1]⁺: 595 fluorophenyl)amino]propoxy}phenyl)- propionic acid I_450 IIa_394 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.269 A {3-[cyclopropanecarbonyl-(2- MS [M + 1]⁺: 581 fluorophenyl)amino]propoxy}phenyl)- propionic acid I_451 IIa_395 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.451 A {3-[(2-fluorophenyl)isobutyrylamino]- MS [M + 1]⁺: 583 propoxy}phenyl)propionic acid I_452 II_55 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.216 A {2-[cyclohexylmethyl-(2-fluorophenyl)- MS [M + 1]⁺: 595 amino]ethoxy}phenyl)propionic acid I_453 II_56 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.146 A {2-[(3-chlorophenyl)- MS [M + 1]⁺: 597, 599 cyclopentylmethylamino]ethoxy}- phenyl)propionic acid I_454 II_57 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.757 A {3-[cyclobutylmethyl-(3-fluorophenyl)- MS [M + 1]⁺: 581 amino]propoxy}phenyl)propionic acid I_455 II_58 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.973 A (cyclobutylmethyl-m-tolylamino)- MS [M + 1]⁺: 577 propoxy]phenyl}propionic acid I_456 II_59 (R)-2-(2-Benzoylphenylamino)-3-{4- rt: 9.268 A [2-(benzylphenylamino)ethoxy]- MS [M + 1]⁺: 571 phenyl}propionic acid I_457 II_60 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.276 A {2-[(2-chlorophenyl)- MS [M + 1]⁺: 597, 599 cyclopentylmethylamino]ethoxy}- phenyl)propionic acid I_458 II_61 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.166 A {2-[(2-fluorophenyl)thiophen-2- MS [M + 1]⁺: 595 ylmethylamino]ethoxy}phenyl)- propionic acid I_459 II_62 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.755 A {3-[(2-fluorophenyl)isobutylamino]- MS [M + 1]⁺: 569 propoxy}phenyl)propionic acid I_460 II_63 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 10.09 A {3-[cyclopentylmethyl-(2- MS [M + 1]⁺: 595 fluorophenyl)amino]propoxy}phenyl)- propionic acid I_461 II_64 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 8.508 A (cyclobutylmethyl-o-tolylamino)- MS [M + 1]⁺: 577 propoxy]phenyl}propionic acid I_462 II_65 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.089 A {2-[(3-fluorophenyl)thiophen-2- MS [M + 1]⁺: 595 ylmethylamino]ethoxy}phenyl)- propionic acid I_463 II_66 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 9.325 A (thiophen-2-ylmethyl-m-tolylamino)- MS [M + 1]⁺: 591 ethoxy]phenyl}propionic acid I_464 II_67 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 9.412 A (thiophen-3-ylmethyl-m-tolylamino)- MS [M + 1]⁺: 605 propoxy]phenyl}propionic acid methyl ester I_465 II_68 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 9.242 A (furan-2-ylmethyl-m-tolylamino)- MS [M + 1]⁺: 589 propoxy]phenyl}propionic acid I_466 II_69 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 9.077 A {2-[(4-fluorophenyl)thiophen-2- MS [M + 1]⁺: 595 ylmethylamino]ethoxy}phenyl)- propionic acid I_467 II_70 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 9.11 A (phenylthiophen-2-ylmethylamino)- MS [M + 1]⁺: 577 ethoxy]phenyl}propionic acid I_468 II_71 (S)-2-(2-Benzoylphenylamino)-3-{4-[3- rt: 9.251 A (phenylthiophen-2-ylmethylamino)- MS [M + 1]⁺: 591 propoxy]phenyl}propionic acid I_469 IIa_396 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.751 A {2-[benzyl-(3-methoxypropionyl)- MS [M + 1]⁺: 581 amino]ethoxy}phenyl)propionic acid I_470 IIa_397 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.849 A {3-[benzyl-(3-methoxypropionyl)- MS [M + 1]⁺: 595 amino]propoxy}phenyl)propionic acid I_471 IIa_398 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.665 A {2-[(3-methoxypropionyl)- MS [M + 1]⁺: 567 phenylamino]ethoxy}phenyl)propionic acid I_472 IIa_399 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.85 A {3-[(3-methoxypropionyl)- MS [M + 1]⁺: 581 phenylamino]propoxy}phenyl)- propionic acid I_473 IIa_400 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.169 A {3-[(2-fluorophenyl)propionylamino]- MS [M + 1]⁺: 569 propoxy}phenyl)propionic acid I_474 IIa_401 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.514 A {3-[(2-fluorophenyl)pent-4- MS [M + 1]⁺: 595 enoylamino]propoxy}phenyl)propionic acid I_475 IIa_402 (S)-3-(4-{3-[Acryloyl-(2-fluorophenyl)- rt: 8.046 A amino]propoxy}phenyl)-2-(2- MS [M + 1]⁺: 567 benzoylphenylamino)propionic acid I_476 IIa_403 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.208 A {3-[but-2-(E)-enoyl-(2-fluorophenyl)- MS [M + 1]⁺: 581 amino]propoxy}phenyl)propionic acid I_477 IIa_404 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.701 A {3-[(2-fluorophenyl)-(3-methylbutyryl)- MS [M + 1]⁺: 597 amino]propoxy}phenyl)propionic acid I_478 IIa_405 (R)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.24 A {2-[phenyl(thiophene-2-carbonyl)- MS [M + 1]⁺: 579 amino]ethoxy}phenyl)propionic acid I_479 IIa_406 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.243 A {3-[(2-fluorophenyl)-(2- MS [M + 1]⁺: 581 methylacryloyl)amino]propoxy}- phenyl)propionic acid I_480 IIa_407 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.232 A {3-[(3-fluorophenyl)-(2- MS [M + 1]⁺: 581 methylacryloyl)amino]propoxy}- phenyl)propionic acid I_481 IIa_408 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.038 A {2-[but-2-(E)-enoyl-(2- MS [M + 1]⁺: 579 methoxyphenyl)amino]ethoxy}phenyl)- propionic acid I_482 IIa_409 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.053 A {2-[but-2-(E)-enoyl-(3- MS [M + 1]⁺: 579 methoxyphenyl)amino]ethoxy}phenyl)- propionic acid I_483 IIa_410 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.541 A {2-[(2-methoxyphenyl)-(3- MS [M + 1]⁺: 595 methylbutyryl)amino]ethoxy}phenyl)- propionic acid I_484 IIa_411 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.701 A {3-[(3-fluorophenyl)-(3-methylbutyryl)- MS [M + 1]⁺: 597 amino]propoxy}phenyl)propionic acid I_485 IIa_412 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.479 A {2-[(3-methoxyphenyl)-(3- MS [M + 1]⁺: 595 methylbutyryl)amino]ethoxy}phenyl)- propionic acid I_486 IIa_413 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.513 A {3-[(3-fluorophenyl)pent-4- MS [M + 1]⁺: 595 enoylamino]propoxy}phenyl)propionic acid I_487 IIa_414 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.596 A {3-[cyclobutanecarbonyl-(3- MS [M + 1]⁺: 595 fluorophenyl)amino]propoxy}phenyl)- propionic acid I_488 IIa_415 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.583 A {3-[cyclobutanecarbonyl-(4- MS [M + 1]⁺: 595 fluorophenyl)amino]propoxy}phenyl)- propionic acid I_489 IIa_416 (R)-2-(2-Benzoylphenylamino)-3-{4- rt: 8.416 A [2-(cyclobutanecarbonylphenylamino)- MS [M + 1]⁺: 563 ethoxy]phenyl}propionic acid I_490 IIa_417 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.082 A {2-[cyclopropanecarbonyl-(2- MS [M + 1]⁺: 579 methoxyphenyl)amino]ethoxy}phenyl)- propionic acid I_491 IIa_418 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.313 A {3-[cyclopropanecarbonyl-(3- MS [M + 1]⁺: 581 fluorophenyl)amino]propoxy}phenyl)- propionic acid I_492 IIa_419 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.293 A {3-[cyclopropanecarbonyl-(4- MS [M + 1]⁺: 581 fluorophenyl)amino]propoxy}phenyl)- propionic acid I_493 IIa_420 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.996 A {2-[(2-methoxyphenyl)- MS [M + 1]⁺: 567 propionylamino]ethoxy}phenyl)- propionic acid I_494 IIa_421 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.175 A {3-[(3-fluorophenyl)propionylamino]- MS [M + 1]⁺: 569 propoxy}phenyl)propionic acid I_495 IIa_422 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.947 A {2-[(3-methoxyphenyl)- MS [M + 1]⁺: 567 propionylamino]ethoxy}phenyl)- propionic acid I_496 IIa_423 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.16 A {3-[(4-fluorophenyl)propionylamino]- MS [M + 1]⁺: 569 propoxy}phenyl)propionic acid I_497 IIa_424 (R)-2-(2-Benzoylphenylamino)-3-{4- rt: 7.952 A [2-(phenylpropionylamino)ethoxy]- MS [M + 1]⁺: 593 phenyl}propionic acid I_498 IIa_425 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.434 A {3-[(3-fluorophenyl)isobutyrylamino]- MS [M + 1]⁺: 583 propoxy}phenyl)propionic acid I_499 IIa_426 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.218 A {2-[isobutyryl-(3-methoxyphenyl)- MS [M + 1]⁺: 581 amino]ethoxy}phenyl)propionic acid I_500 IIa_427 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.424 A {3-[(4-fluorophenyl)isobutyrylamino]- MS [M + 1]⁺: 583 propoxy}phenyl)propionic acid I_501 IIa_428 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.73 A {3-[(2-fluorophenyl)pentanoylamino]- MS [M + 1]⁺: 597 propoxy}phenyl)propionic acid I_502 IIa_429 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.726 A {3-[(3-fluorophenyl)pentanoylamino]- MS [M + 1]⁺: 597 propoxy}phenyl)propionic acid I_503 IIa_430 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.274 A {2-[butyryl-(2-methoxyphenyl)amino]- MS [M + 1]⁺: 581 ethoxy}phenyl)propionic acid I_504 IIa_431 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.447 A {3-[butyryl-(3-fluorophenyl)amino]- MS [M + 1]⁺: 583 propoxy}phenyl)propionic acid I_505 IIa_432 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.222 A {2-[butyryl-(3-methoxyphenyl)amino]- MS [M + 1]⁺: 581 ethoxy}phenyl)propionic acid I_506 IIa_433 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.436 A {3-[butyryl-(4-fluorophenyl)amino]- MS [M + 1]⁺: 583 propoxy}phenyl)propionic acid I_507 IIa_434 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.792 A {3-[(2,2-dimethylpropionyl)-(2- MS [M + 1]⁺: 597 fluorophenyl)amino]propoxy}phenyl)- propionic acid I_508 IIa_435 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.656 A {2-[(2,2-dimethylpropionyl)-(2- MS [M + 1]⁺: 595 methoxyphenyl)amino]ethoxy}phenyl)- propionic acid I_509 IIa_436 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.784 A {3-[(2,2-dimethylpropionyl)-(3- MS [M + 1]⁺: 597 fluorophenyl)amino]propoxy}phenyl)- propionic acid I_510 IIa_437 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.61 A {2-[(2,2-dimethylpropionyl)-(3- MS [M + 1]⁺: 595 methoxyphenyl)amino]ethoxy}phenyl)- propionic acid I_511 IIa_438 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.483 A {2-[isobutyryl-(3- MS [M + 1]⁺: 597 methylsulfanylphenyl)amino]ethoxy}- phenyl)propionic acid I_512 IIa_439 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.122 A {3-[(2-methoxyphenyl)- MS [M + 1]⁺: 581 propionylamino]propoxy}phenyl)- propionic acid I_513 IIa_440 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.213 A {3-[cyclopropanecarbonyl-(2- MS [M + 1]⁺: 593 methoxyphenyl)amino]propoxy}- phenyl)propionic acid I_514 IIa_441 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.385 A {3-[isobutyryl-(2-methoxyphenyl)- MS [M + 1]⁺: 595 amino]propoxy}phenyl)propionic acid I_515 IIa_442 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.159 A {3-[but-2-(E)-enoyl-(2- MS [M + 1]⁺: 593 methoxyphenyl)amino]propoxy}- phenyl)propionic acid I_516 IIa_443 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.163 A {3-[(2-methoxyphenyl)-(2- MS [M + 1]⁺: 593 methylacryloyl)amino]propoxy}- phenyl)propionic acid I_517 IIa_444 (S)-3-(4-{3-[Acryloyl-(2- rt: 8.015 A methoxyphenyl)amino]propoxy}- MS [M + 1]⁺: 579 phenyl)-2-(2-benzoylphenylamino)- propionic acid I_518 IIa_445 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.395 A {3-[butyryl-(2-methoxyphenyl)amino]- MS [M + 1]⁺: 595 propoxy}phenyl)propionic acid I_519 IIa_446 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.111 A {3-[(3-methoxyphenyl)- MS [M + 1]⁺: 581 propionylamino]propoxy}phenyl)- propionic acid I_520 IIa_447 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.246 A {3-[cyclopropanecarbonyl-(3- MS [M + 1]⁺: 593 methoxyphenyl)amino]propoxy}- phenyl)propionic acid I_521 IIa_448 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.374 A {3-[isobutyryl-(3-methoxyphenyl)- MS [M + 1]⁺: 595 amino]propoxy}phenyl)propionic acid I_522 IIa_449 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.204 A {3-[but-2-(E)-enoyl-(3- MS [M + 1]⁺: 593 methoxyphenyl)amino]propoxy}- phenyl)propionic acid I_523 IIa_450 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.134 A {3-[(3-methoxyphenyl)-(2- MS [M + 1]⁺: 593 methylacryloyl)amino]propoxy}- phenyl)propionic acid I_524 IIa_451 (S)-3-(4-{3-[Acryloyl-(3- rt: 8.045 A methoxyphenyl)amino]propoxy}- MS [M + 1]⁺: 579 phenyl)-2-(2-benzoylphenylamino)- propionic acid I_525 IIa_452 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.381 A {3-[butyryl-(3-methoxyphenyl)amino]- MS [M + 1]⁺: 595 propoxy}phenyl)propionic acid I_526 IIa_453 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.42 A {2-[cyclobutanecarbonyl-(2- MS [M + 1]⁺: 593 methoxyphenyl)amino]ethoxy}phenyl)- propionic acid I_527 IIa_454 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.27 A {2-[isobutyryl-(2-methoxyphenyl)- MS [M + 1]⁺: 581 amino]ethoxy}phenyl)propionic acid I_528 IIa_455 (S)-3-{4-[2-(Acryloylnaphthalen-1- rt: 8.35 A ylamino)ethoxy]phenyl}-2-(2- MS [M + 1]⁺: 585 benzoylphenylamino)propionic acid I_529 IIa_456 (S)-3-{4-[2-(Acryloylnaphthalen-2- rt: 8.418 A ylamino)ethoxy]phenyl}-2-(2- MS [M + 1]⁺: 585 benzoylphenylamino)propionic acid I_530 IIa_457 (S)-3-(4-{2-[Acryloyl-(3- rt: 8.172 A methylsulfanylphenyl)amino]ethoxy}- MS [M + 1]⁺: 581 phenyl)-2-(2-benzoylphenylamino)- propionic acidr I_531 IIa_458 (S)-3-(4-{2-[Acryloyl-(4- rt: 8.182 A methylsulfanylphenyl)amino]ethoxy}- MS [M + 1]⁺: 581 phenyl)-2-(2-benzoylphenylamino)- propionic acid I_532 IIa_459 (S)-3-(4-{3-[Acryloyl-(3-fluorophenyl)- rt: 8.098 A amino]propoxy}phenyl)-2-(2- MS [M + 1]⁺: 567 benzoylphenylamino)propionic acid I_533 IIa_460 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.274 A {3-[but-2-(E)-enoyl-(3-fluorophenyl)- MS [M + 1]⁺: 581 amino]propoxy}phenyl)propionic acid I_534 IIa_461 (S)-3-(4-{2-[Acryloyl-(2- rt: 7.886 A methoxyphenyl)amino]ethoxy}phenyl)- MS [M + 1]⁺: 565 2-(2-benzoylphenylamino)propionic acid I_535 IIa_462 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.037 A {2-[(2-methoxyphenyl)-(2- MS [M + 1]⁺: 579 methylacryloyl)amino]ethoxy}phenyl)- propionic acid I_536 IIa_463 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.081 A {2-[cyclopropanecarbonyl-(3- MS [M + 1]⁺: 579 methoxyphenyl)amino]ethoxy}phenyl)- propionic acid I_537 IIa_464 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.384 A {2-[cyclobutanecarbonyl-(3- MS [M + 1]⁺: 593 methoxyphenyl)amino]ethoxy}phenyl)- propionic acid I_538 IIa_465 (S)-3-(4-{2-[Acryloyl-(3- rt: 7.884 A methoxyphenyl)amino]ethoxy}phenyl)- MS [M + 1]⁺: 565 2-(2-benzoylphenylamino)propionic acid I_539 IIa_466 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.975 A {2-[(3-methoxyphenyl)-(2- MS [M + 1]⁺: 579 methylacryloyl)amino]ethoxy}phenyl)- propionic acid I_540 IIa_467 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.236 A {2-[ethyl(naphthalene-2-carbonyl)- MS [M + 1]⁺: 587 amino]ethoxy}phenyl)propionic acid I_541 IIa_468 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.511 A {2-[(naphthalene-2-carbonyl)- MS [M + 1]⁺: 601 propylamino]ethoxy}phenyl)propionic acid I_542 IIa_469 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.881 A {2-[ethyl(quinoline-2-carbonyl)amino]- MS [M + 1]⁺: 588 ethoxy}phenyl)propionic acid I_543 IIa_470 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.2 A {2-[propyl(quinoline-2-carbonyl)- MS [M + 1]⁺: 602 amino]ethoxy}phenyl)propionic acid I_544 IIa_471 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.756 A {2-[ethyl(quinoxaline-2-carbonyl)- MS [M + 1]⁺: 589 amino]ethoxy}phenyl)propionic acid I_545 IIa_472 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.077 A {2-[propyl(quinoxaline-2-carbonyl)- MS [M + 1]⁺: 603 amino]ethoxy}phenyl)propionic acid I_546 IIa_473 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.732 A {2-[ethyl(thiophene-2-carbonyl)- MS [M + 1]⁺: 543 amino]ethoxy}phenyl)propionic acid I_547 IIa_474 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.04 A {2-[propyl(thiophene-2-carbonyl)- MS [M + 1]⁺: 557 amino]ethoxy}phenyl)propionic acid I_548 IIa_475 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 6.713 A {2-[ethyl(pyridine-3-carbonyl)amino]- MS [M + 1]⁺: 538 ethoxy}phenyl)propionic acid I_549 IIa_476 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.037 A {2-[propyl(pyridine-3-carbonyl)amino]- MS [M + 1]⁺: 552 ethoxy}phenyl)propionic acid I_550 IIa_477 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 7.924 A {2-[ethyl-(3-thiophen-2-ylacryloyl)- MS [M + 1]⁺: 569 amino]ethoxy}phenyl)propionic acid I_551 IIa_478 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.236 A {2-[propyl-(3-thiophen-2-ylacryloyl)- MS [M + 1]⁺: 583 amino]ethoxy}phenyl)propionic acid I_552 IIa_479 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.572 A {2-[(3,3-dimethylbutyryl)propylamino]- MS [M + 1]⁺: 545 ethoxy}phenyl)propionic acid I_553 IIa_480 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 5.866 A {2-[ethyl-(3-pyridin-3-ylpropionyl)- MS [M + 1]⁺: 566 amino]ethoxy}phenyl)propionic acid I_554 IIa_481 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 6.125 A {2-[propyl-(3-pyridin-3-ylpropionyl)- MS [M + 1]⁺: 580 amino]ethoxy}phenyl)propionic acid I_555 IIa_482 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.138 A (cyclobutanecarbonylpropylamino)- MS [M + 1]⁺: 529 ethoxy]phenyl}propionic acid I_556 IIa_483 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 7.963 A (isobutyrylpropylamino)ethoxy]- MS [M + 1]⁺: 517 phenyl}propionic acid I_557 IIa_484 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 7.945 A (butyrylpropylamino)ethoxy]phenyl}- MS [M + 1]⁺: 517 propionic acid I_558 IIa_485 (S)-3-{4-[2-(Benzoylethylamino)- rt: 7.725 A ethoxy]phenyl}-2-(2- MS [M + 1]⁺: 537 benzoylphenylamino)propionic acid I_559 IIa_486 (S)-2-(2-Benzoylphenylamino)-3-{4-[2- rt: 8.03 A (benzoylpropylamino)ethoxy]phenyl}- MS [M + 1]⁺: 551 propionic acid I_560 IIa_487 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.034 A {2-[ethyl-(3-phenylacryloyl)amino]- MS [M + 1]⁺: 563 ethoxy}phenyl)propionic acid I_561 IIa_488 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.102 A {2-[(2,2-dimethylpropionyl)- MS [M + 1]⁺: 517 ethylamino]ethoxy}phenyl)propionic acid I_562 IIa_489 (S)-2-(2-Benzoylphenylamino)-3-(4- rt: 8.44 A {2-[(2,2-dimethylpropionyl)- MS [M + 1]⁺: 531 propylamino]ethoxy}phenyl)propionic acid 

1. A method for the treatment or prevention of diseases mediated by PPARγ comprising the administration to a mammal of an effective amount of a compound of formula I

its stereoisomers and mixtures thereof, its polymorphs and mixtures thereof, and the pharmaceutically acceptable solvates and addition salts of all of them, wherein R1 represents the radical 2-benzoylphenylamino; R2 represents —(CH₂)_(s)—N(COR3)-A-J-T or —(CH₂)_(s)—N(R4)-B-J-T; R3 represents —(C₁-C₁₀)alkyl optionally substituted by one or more substituents selected from —F, —Cl, —Br and —O(C₁-C₄)alkyl; —(C₂-C₆)alkenyl; —(C₂-C₆)alkynyl; —(C₁-C₃)alkylene-Y; —(C₂-C₃)alkenylene-Y; —(C₂-C₃)alkynylene-Y or —Y; R4 represents —(C₄-C₁₀)alkyl optionally substituted by one or more substituents selected from —F, —Cl, —Br and —O(C₁-C₄)alkyl; —(C₂-C₆)alkenyl; —(C₂-C₆)alkynyl; —(C₁-C₄)alkylene-Y; —(C₂-C₄)alkenylene-Y; —(C₂-C₄)alkynylene-Y or —Y; s represents 2 or 3; A represents —(C₁-C₄)alkylene-; —(C₂-C₄)alkenylene-; —(C₂-C₄)alkynylene-; —(C₁-C₄)alkylene-Z-, wherein the alkylene part is attached to the N atom and Z is attached to J; or -Z-; B represents —(C₄)alkylene-; —(C₂-C₄)alkenylene-; —(C₂-C₄)alkynylene-; —(C₁-C₄)alkylene-Z-, wherein the alkylene part is attached to the N atom and Z is attached to J; or -Z-; J represents a single bond or a biradical selected from the following groups: a) —(CH₂)₁₋₄—, —O—, —S—, —SO—, —SO₂—, —CO—, —OCO—, —COO—, —OCONR5-, —NR5COO—, —CONR5-, —NR5CO—, —NR5-, —NR5SO₂—, —SO₂NR5-; and b) —O(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-O—, —S(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-S—, —SO(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-SO—, —SO₂(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-SO₂—, —OCO—(C₁-C₄)alkyl-, —COO—(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-OCO—, —(C₁-C₄)alkyl-COO—, —OCONR5-(C₁-C₄)alkyl-, —NR5COO—(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-OCONR5-, —(C₁-C₄)alkyl-NR5COO—, —CONR5-(C₁-C₄)alkyl-, —NR5CO—(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-CONR5-, —(C₁-C₄)alkyl-NR5CO—, —NR5-(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-NR5-, —SO₂NR5-(C₁-C₄)alkyl-, —NR5SO₂—(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-SO₂NR5-, —(C₁-C₄)alkyl-NR5SO₂—; T represents —H, —(C₁-C₄)alkyl, —(C₂-C₄)alkenyl, —(C₂-C₄)alkynyl or —Y; Y represents a monoradical coming from a cycle selected from a (C₃-C₆)cycloalkane, cyclohexene, a heterocycle, benzene and a bicycle, wherein all these cycles can be optionally substituted with one or more substituents selected from the group —OH, —CHO, —SH, —NO₂, —CN, —F, —Cl, —Br, —CO(C₁-C₄)alkyl, —COO(C₁-C₄)alkyl, —OCO(C₁-C₄)alkyl, —S(C₁-C₄)alkyl, —SO(C₁-C₄)alkyl, —SO₂(C₁-C₄)alkyl, —SO₂—O(C₁-C₄)alkyl, —O—SO₂(C₁-C₄)alkyl, —NR5R6, —CONR5R6, —(C₁-C₄)alkyl optionally substituted by one or more —OH or —F and —O(C₁-C₄)alkyl optionally substituted by one or more —OH or —F, and wherein the cycles (C₃-C₆)cycloalkane, cyclohexene and bicycle can also be optionally substituted with one or more substituents oxo (═O); Z represents a biradical coming from a cycle selected from a (C₃-C₆)cycloalkane, cyclohexene, a heterocycle, benzene and a bicycle, wherein all these cycles can be optionally substituted with one or more substituents selected from the group —OH, —CHO, —SH, —NO₂, —CN, —F, —Cl, —Br, —CO(C₁-C₄)alkyl, —COO(C₁-C₄)alkyl, —OCO(C₁-C₄)alkyl, —S(C₁-C₄)alkyl, —SO(C₁-C₄)alkyl, —SO₂(C₁-C₄)alkyl, —SO₂—O(C₁-C₄)alkyl, —O—SO₂(C₁-C₄)alkyl, —NR5R6, —CONR5R6, —(C₁-C₄)alkyl optionally substituted by one or more —OH or —F and —O(C₁-C₄)alkyl optionally substituted by one or more —OH or —F, and wherein the cycles (C₃-C₆)cycloalkane, cyclohexene and bicycle can also be optionally substituted with one or more substituents oxo (═O); R5 and R6 independently represent —H or —(C₁-C₄)alkyl; a heterocycle in the above definitions represents a five- or six-membered aromatic ring containing from one to three heteroatoms independently selected from O, S and N, wherein said ring can be attached to the rest of the molecule through a carbon or a nitrogen atom; and a bicycle in the above definitions represents a partially unsaturated, saturated or aromatic seven- to ten-membered ring optionally containing from one to three heteroatoms independently selected from O, S and N, wherein said ring or rings can be attached to the rest of the molecule through a carbon or a nitrogen atom.
 2. A method for the treatment or prevention of metabolic diseases comprising the administration to a mammal of an effective amount of a compound of formula I

its stereoisomers and mixtures thereof, its polymorphs and mixtures thereof, and the pharmaceutically acceptable solvates and addition salts of all of them, wherein R1 represents the radical 2-benzoylphenylamino; R2 represents —(CH₂)_(s)—N(COR3)-A-J-T or —(CH₂)_(s)—N(R4)-B-J-T; R3 represents —(C₁-C₁₀)alkyl optionally substituted by one or more substituents selected from —F, —Cl, —Br and —O(C₁-C₄)alkyl; —(C₂-C₆)alkenyl; —(C₂-C₆)alkynyl; —(C₁-C₃)alkylene-Y; —(C₂-C₃)alkenylene-Y; —(C₂-C₃)alkynylene-Y or —Y; R4 represents —(C₄-C₁₀)alkyl optionally substituted by one or more substituents selected from —F, —Cl, —Br and —O(C₁-C₄)alkyl; —(C₂-C₆)alkenyl; —(C₂-C₆)alkynyl; —(C₁-C₄)alkylene-Y; —(C₂-C₄)alkenylene-Y; —(C₂-C₄)alkynylene-Y or —Y; s represents 2 or 3; A represents —(C₁-C₄)alkylene-; —(C₂-C₄)alkenylene-; —(C₂-C₄)alkynylene-; —(C₁-C₄)alkylene-Z-, wherein the alkylene part is attached to the N atom and Z is attached to J; or -Z-; B represents —(C₄)alkylene-; —(C₂-C₄)alkenylene-; —(C₂-C₄)alkynylene-; —(C₁-C₄)alkylene-Z-, wherein the alkylene part is attached to the N atom and Z is attached to J; or -Z-; J represents a single bond or a biradical selected from the following groups: a) —(CH₂)₁₋₄—, —O—, —S—, —SO—, —SO₂—, —CO—, —OCO—, —COO—, —OCONR5-, —NR5COO—, —CONR5-, —NR5CO—, —NR5-, —NR5SO₂—, —SO₂NR5-; and b) —O(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-O—, —S(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-S—, —SO(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-SO—, —SO₂(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-SO₂—, —OCO—(C₁-C₄)alkyl-, —COO—(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-OCO—, —(C₁-C₄)alkyl-COO—, —OCONR5-(C₁-C₄)alkyl-, —NR5COO—(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-OCONR5-, —(C₁-C₄)alkyl-NR5COO—, —CONR5-(C₁-C₄)alkyl-, —NR5CO—(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-CONR5-, —(C₁-C₄)alkyl-NR5CO—, —NR5-(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-NR5-, —SO₂NR5-(C₁-C₄)alkyl-, —NR5SO₂—(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-SO₂NR5-, —(C₁-C₄)alkyl-NR5SO₂—; T represents —H, —(C₁-C₄)alkyl, —(C₂-C₄)alkenyl, —(C₂-C₄)alkynyl or —Y; Y represents a monoradical coming from a cycle selected from a (C₃-C₆)cycloalkane, cyclohexene, a heterocycle, benzene and a bicycle, wherein all these cycles can be optionally substituted with one or more substituents selected from the group —OH, —CHO, —SH, —NO₂, —CN, —F, —Cl, —Br, —CO(C₁-C₄)alkyl, —COO(C₁-C₄)alkyl, —OCO(C₁-C₄)alkyl, —S(C₁-C₄)alkyl, —SO(C₁-C₄)alkyl, —SO₂(C₁-C₄)alkyl, —SO₂—O(C₁-C₄)alkyl, —O—SO₂(C₁-C₄)alkyl, —NR5R6, —CONR5R6, —(C₁-C₄)alkyl optionally substituted by one or more —OH or —F and —O(C₁-C₄)alkyl optionally substituted by one or more —OH or —F, and wherein the cycles (C₃-C₆)cycloalkane, cyclohexene and bicycle can also be optionally substituted with one or more substituents oxo (═O); Z represents a biradical coming from a cycle selected from a (C₃-C₆)cycloalkane, cyclohexene, a heterocycle, benzene and a bicycle, wherein all these cycles can be optionally substituted with one or more substituents selected from the group —OH, —CHO, —SH, —NO₂, —CN, —F, —Cl, —Br, —CO(C₁-C₄)alkyl, —COO(C₁-C₄)alkyl, —OCO(C₁-C₄)alkyl, —S(C₁-C₄)alkyl, —SO(C₁-C₄)alkyl, —SO₂(C₁-C₄)alkyl, —SO₂—O(C₁-C₄)alkyl, —O—SO₂(C₁-C₄)alkyl, —NR5R6, —CONR5R6, —(C₁-C₄)alkyl optionally substituted by one or more —OH or —F and —O(C₁-C₄)alkyl optionally substituted by one or more —OH or —F, and wherein the cycles (C₃-C₆)cycloalkane, cyclohexene and bicycle can also be optionally substituted with one or more substituents oxo (═O); R5 and R6 independently represent —H or —(C₁-C₄)alkyl; a heterocycle in the above definitions represents a five- or six-membered aromatic ring containing from one to three heteroatoms independently selected from O, S and N, wherein said ring can be attached to the rest of the molecule through a carbon or a nitrogen atom; and a bicycle in the above definitions represents a partially unsaturated, saturated or aromatic seven- to ten-membered ring optionally containing from one to three heteroatoms independently selected from O, S and N, wherein said ring or rings can be attached to the rest of the molecule through a carbon or a nitrogen atom.
 3. A method according to claim 2, wherein the metabolic disease is selected from non-insulin-dependent diabetes mellitus and obesity.
 4. A method for the treatment or prevention of cardiovascular diseases associated with metabolic syndrome, inflammatory diseases, cancer, bone diseases, skin wound healing, cutaneous disorders associated with an anomalous differentiation of epidermic cells and other disorders where insulin resistance is a component, comprising the administration to a mammal of an effective amount of a compound of formula I

its stereoisomers and mixtures thereof, its polymorphs and mixtures thereof, and the pharmaceutically acceptable solvates and addition salts of all of them, wherein R1 represents the radical 2-benzoylphenylamino; R2 represents —(CH₂)_(s)—N(COR3)-A-J-T or —(CH₂)_(s)—N(R4)-B-J-T; R3 represents —(C₁-C₁₀)alkyl optionally substituted by one or more substituents selected from —F, —Cl, —Br and —O(C₁-C₄)alkyl; —(C₂-C₆)alkenyl; —(C₂-C₆)alkynyl; —(C₁-C₃)alkylene-Y; —(C₂-C₃)alkenylene-Y; —(C₂-C₃)alkynylene-Y or —Y; R4 represents —(C₄-C₁₀)alkyl optionally substituted by one or more substituents selected from —F, —Cl, —Br and —O(C₁-C₄)alkyl; —(C₂-C₆)alkenyl; —(C₂-C₆)alkynyl; —(C₁-C₄)alkylene-Y; —(C₂-C₄)alkenylene-Y; —(C₂-C₄)alkynylene-Y or —Y; s represents 2 or 3; A represents —(C₁-C₄)alkylene-; —(C₂-C₄)alkenylene-; —(C₂-C₄)alkynylene-; —(C₁-C₄)alkylene-Z-, wherein the alkylene part is attached to the N atom and Z is attached to J; or -Z-; B represents —(C₄)alkylene-; —(C₂-C₄)alkenylene-; —(C₂-C₄)alkynylene-; —(C₁-C₄)alkylene-Z-, wherein the alkylene part is attached to the N atom and Z is attached to J; or -Z-; J represents a single bond or a biradical selected from the following groups: a) —(CH₂)₁₋₄—, —O—, —S—, —SO—, —SO₂—, —CO—, —OCO—, —COO—, —OCONR5-, —NR5COO—, —CONR5-, —NR5CO—, —NR5-, —NR5SO₂—, —SO₂NR5-; and b) —O(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-O—, —S(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-S—, —SO(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-SO—, —SO₂(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-SO₂—, —OCO—(C₁-C₄)alkyl-, —COO—(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-OCO—, —(C₁-C₄)alkyl-COO—, —OCONR5-(C₁-C₄)alkyl-, —NR5COO—(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-OCONR5-, —(C₁-C₄)alkyl-NR5COO—, —CONR5-(C₁-C₄)alkyl-, —NR5CO—(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-CONR5-, —(C₁-C₄)alkyl-NR5CO—, —NR5-(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-NR5-, —SO₂NR5-(C₁-C₄)alkyl-, —NR5SO₂—(C₁-C₄)alkyl-, —(C₁-C₄)alkyl-SO₂NR5-, —(C₁-C₄)alkyl-NR5SO₂—; T represents —H, —(C₁-C₄)alkyl, —(C₂-C₄)alkenyl, —(C₂-C₄)alkynyl or —Y; Y represents a monoradical coming from a cycle selected from a (C₃-C₆)cycloalkane, cyclohexene, a heterocycle, benzene and a bicycle, wherein all these cycles can be optionally substituted with one or more substituents selected from the group —OH, —CHO, —SH, —NO₂, —CN, —F, —Cl, —Br, —CO(C₁-C₄)alkyl, —COO(C₁-C₄)alkyl, —OCO(C₁-C₄)alkyl, —S(C₁-C₄)alkyl, —SO(C₁-C₄)alkyl, —SO₂(C₁-C₄)alkyl, —SO₂—O(C₁-C₄)alkyl, —O—SO₂(C₁-C₄)alkyl, —NR5R6, —CONR5R6, —(C₁-C₄)alkyl optionally substituted by one or more —OH or —F and —O(C₁-C₄)alkyl optionally substituted by one or more —OH or —F, and wherein the cycles (C₃-C₆)cycloalkane, cyclohexene and bicycle can also be optionally substituted with one or more substituents oxo (═O); Z represents a biradical coming from a cycle selected from a (C₃-C₆)cycloalkane, cyclohexene, a heterocycle, benzene and a bicycle, wherein all these cycles can be optionally substituted with one or more substituents selected from the group —OH, —CHO, —SH, —NO₂, —CN, —F, —Cl, —Br, —CO(C₁-C₄)alkyl, —COO(C₁-C₄)alkyl, —OCO(C₁-C₄)alkyl, —S(C₁-C₄)alkyl, —SO(C₁-C₄)alkyl, —SO₂(C₁-C₄)alkyl, —SO₂—O(C₁-C₄)alkyl, —O—SO₂(C₁-C₄)alkyl, —NR5R6, —CONR5R6, —(C₁-C₄)alkyl optionally substituted by one or more —OH or —F and —O(C₁-C₄)alkyl optionally substituted by one or more —OH or —F, and wherein the cycles (C₃-C₆)cycloalkane, cyclohexene and bicycle can also be optionally substituted with one or more substituents oxo (═O); R5 and R6 independently represent —H or —(C₁-C₄)alkyl; a heterocycle in the above definitions represents a five- or six-membered aromatic ring containing from one to three heteroatoms independently selected from O, S and N, wherein said ring can be attached to the rest of the molecule through a carbon or a nitrogen atom; and a bicycle in the above definitions represents a partially unsaturated, saturated or aromatic seven- to ten-membered ring optionally containing from one to three heteroatoms independently selected from O, S and N, wherein said ring or rings can be attached to the rest of the molecule through a carbon or a nitrogen atom. 